Page last updated: 2024-11-04

uridine

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Cross-References

ID SourceID
PubMed CID6029
CHEMBL ID100259
CHEBI ID16704
SCHEMBL ID20667
MeSH IDM0022344

Synonyms (102)

Synonym
CHEMBL100259
MLS000069625 ,
smr000058222
1-beta-d-ribofuranosylpyrimidine-2,4(1h,3h)-dione
1-beta-d-ribofuranosyluracil
CHEBI:16704 ,
beta-uridine
1-[(2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]pyrimidine-2,4-dione
arau
uracil riboside
1-.beta.-d-ribofuranosyluracil
nsc-20256
uridin
nsc20256
urd ,
SMP1_000029
58-96-8
uridine ,
C00299
uridine, bioultra, >=99%
uridine, powder, bioreagent, suitable for cell culture
uridine, >=99%
DB02745
1AF2
NCGC00142368-01
nsc 20256
einecs 200-407-5
ai3-52690
uracil, 1-beta-d-ribofuranosyl-
6B6FA3F8-70A2-44EA-B99C-D35D0A9237AA
bdbm50088517
BMSE000158
U0020
1-[(2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidine-2,4-dione
BMSE000864
BMSE000816
HMS2230P13
NCGC00017312-02
1-[(4s,2r,3r,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-1,3-dihydropyrimi dine-2,4-dione
1-a-d-ribofuranosyluracil
uracil-1-a-d-ribofuranoside
whi7hq7h85 ,
unii-whi7hq7h85
EPITOPE ID:149164
4JX9
S2029
AKOS015896922
gtpl4566
1-[(2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-1,2,3,4-tetrahydropyrimidine-2,4-dione
uridine [usp impurity]
uridine [mi]
uridine [usp-rs]
uridine [mart.]
uridine [who-dd]
adenosine impurity f [ep impurity]
uridine [inci]
1-.beta.-d-ribofuranosylpyrimidine-2,4(1h,3h)-dione
CCG-214447
AM83934
SCHEMBL20667
mfcd00006526
CS-5153
HY-B1449
d-uridine
uracil-1-.beta.-d-ribofuranoside
.beta.-uridine
d-ribosyl uracil
.beta.-d-ribofuranoside, 2,4(1h,3h)-pyrimidinedione-1
1-((2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidine-2,4(1h,3h)-dione
SRI-10895_12
OPERA_ID_118
4PD6
b-uridine
uridine, united states pharmacopeia (usp) reference standard
beta-d-ribofuranosyl-uridine
uridine, vetec(tm) reagent grade, 99%
1-beta-d-ribofuranosylpyrimidine-2,4(1h,3h)-dione (uridine)
NCGC00017312-04
1-b-d-ribofuranosyluracil
1-beta-delta-ribofuranosyl-2,4(1h,3h)-pyrimidinedione
1-beta-delta-ribofuranosyluracil
1-b-d-ribofuranosyl-2,4(1h,3h)-pyrimidinedione
b-d-ribofuranoside 2,4(1h,3h)-pyrimidinedione-1
beta-delta-ribofuranoside 2,4(1h,3h)-pyrimidinedione-1
1-((2r,3r,4s,5r)-tetrahydro-3,4-dihydroxy-5-(hydroxymethyl)furan-2-yl)pyrimidine-2,4(1h,3h)-dione
DTXSID40891555 ,
Q422573
rg2417
DS-14345
uridine,(s)
BRD-K13050303-001-18-1
HMS3884M20
NCGC00017312-05
EN300-221746
uridine (usp-rs)
dtxcid001030648
uridine (usp impurity)
adenosine impurity f (ep impurity)
uridine (mart.)
1-beta-d-ribofuranosyluracil, uracil-1-beta-d-ribofuranoside
Z1741976658
BP-58653

Research Excerpts

Overview

Uridine triacetate is an FDA-approved antidote for 5-fluorouracil or capecitabine overdose and early-onset, life-threatening toxicity. Uridine is a pyrimidine nucleoside that exerts restorative functions in tissues under stress.

ExcerptReferenceRelevance
"Uridine (Urd) is a promising biochemical modulator to reduce host toxicity caused by 5-fluorouracil (5-FU) without impairing its antitumor activity. "( Design of novel potent inhibitors of human uridine phosphorylase-1: synthesis, inhibition studies, thermodynamics, and in vitro influence on 5-fluorouracil cytotoxicity.
Basso, LA; Campos, MM; de Souza, ON; Erig, T; Farias, CB; Machado, P; Renck, D; Roesler, R; Rosado, LA; Santos, DS; Souto, AA; Timmers, LF, 2013
)
2.1
"Uridine (UR) is a pyrimidine nucleoside that plays an important role in regulating glucose and lipid metabolism. "( Uridine attenuates obesity, ameliorates hepatic lipid accumulation and modifies the gut microbiota composition in mice fed with a high-fat diet.
De Jonge, HR; Deng, ZY; Liu, Y; Ruan, Z; Wu, X; Xie, C; Zhai, Z, 2021
)
3.51
"Uridine is a potential endogenous neuromodulator studied for several decades for its antiepileptic effect, but the results were controversial. "( Antiepileptic effect of uridine may be caused by regulating dopamine release and receptor expression in corpus striatum.
Bai, Y; Li, L; Wang, T; Wu, C; Zhang, L; Zhou, X, 2018
)
2.23
"Uridine is a kind of pyrimidine nucleoside that has been widely applied in the pharmaceutical industry. "( Metabolic engineering of Escherichia coli for high-yield uridine production.
Chen, N; Fan, X; Jia, Z; Li, Q; Li, Y; Ma, Q; Wu, H; Xie, X; Xu, Q; Yang, B; Zhang, C, 2018
)
2.17
"Uridine triacetate is an FDA-approved antidote for 5-fluorouracil or capecitabine overdose and early-onset, life-threatening toxicity within 96 h of last chemotherapy dose."( Fluoropyrimidine-induced toxicity and DPD deficiency.. A case report of early onset, lethal capecitabine-induced toxicity and mini review of the literature. Uridine triacetate: Efficacy and safety as an antidote. Is it accessible outside USA?
Amylidi, AL; Angelaki, A; Aravantinos, G; Boumpoucheropoulos, S; Fildissis, G; Lampropoulou, DI; Laschos, K; Nanou, E; Nasioulas, G; Papadopoulou, E; Soupos, N; Zidianakis, V, 2020
)
1.48
"As uridine is a combination of d-ribose and uracil, which have been studied earlier with the same method, this study also considers the effect of chemical environment and the relevant functional groups."( Gas-phase study on uridine: Conformation and X-ray photofragmentation.
Ha, DT; Itälä, E; Kooser, K; Kukk, E; Levola, H; Rachlew, E, 2015
)
1.26
"Uridine is a pyrimidine nucleoside that exerts restorative functions in tissues under stress. "( Chronic Uridine Administration Induces Fatty Liver and Pre-Diabetic Conditions in Mice.
Le, TT; Pizzorno, G; Urasaki, Y, 2016
)
2.31
"Uridine is a natural nucleoside precursor of uridine monophosphate in organisms and thus is considered to be safe and is used in a wide range of clinical settings. "( Uridine homeostatic disorder leads to DNA damage and tumorigenesis.
Cai, C; Cao, D; Cao, Z; Chen, X; Huang, D; Ma, J; Zhang, X; Zhou, B, 2016
)
3.32
"Uridine phosphorylase is a key enzyme in the pyrimidine salvage pathway. "( Glycal formation in crystals of uridine phosphorylase.
Begley, TP; Bu, W; Ealick, SE; O'Leary, SE; Paul, D; Rajashankar, K; Sanders, JM; Settembre, EC; Toms, A, 2010
)
2.09
"Uridine is a therapy for hereditary orotic aciduria and is being investigated in other disorders caused by mitochondrial dysfunction, including toxicities resulting from treatment with nucleoside reverse transcriptase inhibitors in HIV. "( Enhanced uridine bioavailability following administration of a triacetyluridine-rich nutritional supplement.
Cheung, P; Jacob, P; Mulligan, K; Roman, MC; Schambelan, M; Walker, UA; Weinberg, ME; Wen, M, 2011
)
2.23
"Uridine is a pyrimidine nucleoside that plays a crucial role in synthesis of RNA, glycogen, and biomembrane. "( Biochemistry of uridine in plasma.
Koyama, H; Kurajoh, M; Moriwaki, Y; Shoji, T; Tsutsumi, Z; Yamamoto, T, 2011
)
2.16
"Uridine is an interesting candidate in the prevention of NRTI-induced lipoatrophy in vivo."( Uridine abrogates the adverse effects of antiretroviral pyrimidine analogues on adipose cell functions.
Auclair, M; Capeau, J; Caron, M; Kornprobst, M; Lebrecht, D; Walker, UA, 2006
)
2.5
"The uridine bulge, which is an important contributor to the structural stability of TAR, plays an essential role in drug binding."( Binding of Hoechst 33258 to the TAR RNA of HIV-1. Recognition of a pyrimidine bulge-dependent structure.
Bailly, C; Colson, P; Dassonneville, L; Hamy, F; Houssier, C, 1997
)
0.78
"Uridine is an intermediate."( In vitro assessment of salvage pathways for pyrimidine bases in rat liver and brain.
Cappiello, M; Giorgelli, F; Ipata, PL; Mascia, L; Scolozzi, C, 1998
)
1.02
"Uridine is a partial linear competitive inhibitor of UDPglucose and an uncompetitive inhibitor of galactose-1-phosphate."( Effect of uridine on hepatic galactose-1-phosphate uridyltransferase.
Bovee, BW; Rogers, S; Segal, S, 1989
)
1.4
"Uridine was found to be a potent noncompetitive inhibitor of pyrimidine base degradation in vitro, displaying an inhibition constant (Ki) for 5-FU of 0.71 microM."( Effects of uridine and thymidine on the degradation of 5-fluorouracil, uracil, and thymine by rat liver dihydropyrimidine dehydrogenase.
O'Dea, RF; Ramnaraine, ML; Tuchman, M, 1985
)
1.38

Effects

Uridine has a number of biological effects on a variety of organs with or without disease. Uridine metabolism has an important role in the physiopathology of the nervous system.

Uridine has been reported to induce fever in man, thus the USP rabbit pyrogen test predicted for the clinical response. Uridine is an important target for the development of modified nucleoside analogues for pharmaceutical applications.

ExcerptReferenceRelevance
"Uridine has a number of biological effects on a variety of organs with or without disease, such as the reproductive organs, central and peripheral nervous systems, and liver."( Biochemistry of uridine in plasma.
Koyama, H; Kurajoh, M; Moriwaki, Y; Shoji, T; Tsutsumi, Z; Yamamoto, T, 2011
)
1.44
"Uridine metabolism has an important role in the physiopathology of the nervous system. "( Uridine induces differentiation in human neuroblastoma cells via protein kinase C epsilon.
Lauro, GM; Politi, V; Silei, V, 2000
)
3.19
"Uridine has also been an important target for the development of modified nucleoside analogues for pharmaceutical applications."( 5-Halogenation of Uridine Suppresses Protonation-Induced Tautomerization and Enhances Glycosidic Bond Stability of Protonated Uridine: Investigations via IRMPD Action Spectroscopy, ER-CID Experiments, and Theoretical Calculations.
Berden, G; Frieler, CE; Hamlow, LA; Israel, E; Mikawy, NN; Oomens, J; Rodgers, MT; Roy, HA; Zhu, Y, 2022
)
1.78
"Uridine has been widely reported to be effective in regulating lipid metabolism."( Cytidine Alleviates Dyslipidemia and Modulates the Gut Microbiota Composition in ob/ob Mice.
Bai, P; Feng, X; Niu, K; Qiu, F; Zhang, J, 2023
)
1.63
"Uridine has formerly been shown to alleviate obesity and hepatic lipid accumulation. "( N-carbamoyl aspartate reduced body weight by stimulating the thermogenesis of iBAT.
Wang, Z; Wu, X; Zhang, Y; Zhou, T, 2023
)
2.35
"Uridine triacetate has shown promising results for the emergency treatment of patients who either receive an overdose of the cancer treatment fluorouracil or capecitabine or to treat patients who exhibit early-onset, severe, or life-threatening toxicity."( Case report of capecitabine toxicity and use of uridine triacetate.
Duffy, AP; Hausner, PF; Oliver, WD, 2019
)
1.49
"Uridine triacetate has been shown to be an effective antidote against mortality and toxicity caused by either overdoses or exaggerated susceptibility to the widely used anticancer agents 5-fluorouracil (5-FU) and capecitabine. "( Prompt treatment with uridine triacetate improves survival and reduces toxicity due to fluorouracil and capecitabine overdose or dihydropyrimidine dehydrogenase deficiency.
Bamat, MK; Garcia, RAG; Saydoff, JA; von Borstel, RW, 2018
)
2.24
"Uridine prodrug PN401 has been shown to have neuroprotective effects in models of Parkinson's disease and Huntington's disease. "( Uridine prodrug improves memory in Tg2576 and TAPP mice and reduces pathological factors associated with Alzheimer's disease in related models.
Garcia, R; Hu, Z; Li, Q; Olariu, A; Pei, J; Saydoff, JA; Sheng, J; Sun, GY; von Borstel, R, 2013
)
3.28
"Uridine has earlier been show to down modulate inflammation in models of lung inflammation. "( Local but Not Systemic Administration of Uridine Prevents Development of Antigen-Induced Arthritis.
Chalise, JP; Chenna Narendra, S; Magnusson, M; Uppugunduri, S, 2015
)
2.13
"Uridine has the ability to modulate liver metabolism; however, the precise mechanism has not been delineated."( Chronic Uridine Administration Induces Fatty Liver and Pre-Diabetic Conditions in Mice.
Le, TT; Pizzorno, G; Urasaki, Y, 2016
)
1.59
"Uridine (Urd), which has been reported as a major component of RNA, plays an important role in various biological process including neuroprotection, biochemical modulation and glycolysis, although its role in constipation has yet to be established. "( Uridine stimulate laxative effect in the loperamide-induced constipation of SD rats through regulation of the mAChRs signaling pathway and mucin secretion.
Go, J; Hong, JT; Hwang, DY; Kim, JE; Lee, HA; Sung, JE; Yun, WB, 2017
)
3.34
"Uridine has recently been shown to provide clinical benefit in treatment of Alzheimer's disease due to its involvement in increasing number of brain synapses along with other phospholipid precursors."( Long-term cognitive effects of uridine treatment in a neonatal rat model of hypoxic-ischemic encephalopathy.
Alkan, T; Cakir, A; Cansev, M; Goren, B; Kahveci, N; Ocalan, B; Serter Kocoglu, S, 2017
)
1.46
"Uridine has been advocated for the treatment of HIV-1/HAART-associated lipodystrophy (HALS), although its metabolism in HIV-1-infected patients is poorly understood."( Uridine metabolism in HIV-1-infected patients: effect of infection, of antiretroviral therapy and of HIV-1/ART-associated lipodystrophy syndrome.
Andreu, A; Cano-Soldado, P; Domingo, JC; Domingo, P; Fernandez, I; Gallego-Escuredo, JM; Giralt, M; Gutierrez, Mdel M; Marti, R; Mateo, MG; Pastor-Anglada, M; Pomar, V; Torres-Torronteras, J; Vidal, F; Villarroya, F, 2010
)
3.25
"Uridine has a number of biological effects on a variety of organs with or without disease, such as the reproductive organs, central and peripheral nervous systems, and liver."( Biochemistry of uridine in plasma.
Koyama, H; Kurajoh, M; Moriwaki, Y; Shoji, T; Tsutsumi, Z; Yamamoto, T, 2011
)
1.44
"Uridine insertions have been identified in the T loop of tRNALys from Didymium and tRNAGlu from Physarum."( Insertional editing of mitochondrial tRNAs of Physarum polycephalum and Didymium nigripes.
Antes, T; Costandy, H; Mahendran, R; Miller, D; Spottswood, M, 1998
)
1.02
"Uridine metabolism has an important role in the physiopathology of the nervous system. "( Uridine induces differentiation in human neuroblastoma cells via protein kinase C epsilon.
Lauro, GM; Politi, V; Silei, V, 2000
)
3.19
"Both uridine and UTP have been found to be potent inhibitors of brain and ovarian transferase activity."( Modulation of rat tissue galactose-1-phosphate uridyltransferase by uridine and uridine triphosphate.
Rogers, S; Segal, S, 1991
)
0.97
"Uridine has been found to be an inhibitor of the enzyme in in vitro studies and to cause an increase in galactose-1-phosphate in liver perfused with galactose which is consistent with physiologic inhibition of the enzyme."( Effect of uridine on hepatic galactose-1-phosphate uridyltransferase.
Bovee, BW; Rogers, S; Segal, S, 1989
)
1.4
"Uridine has been reported to induce fever in man, thus the USP rabbit pyrogen test predicted for the clinical response."( Uridine-induced hyperthermia in the rabbit.
Ackerman, SK; Chin, TF; Cradock, JC; Hochstein, HD; Vishnuvajjala, BR, 1986
)
2.44
"Uridine kinase has been purified to homogeneity from Ehrlich ascites tumor cells. "( Homogeneous uridine kinase from Ehrlich ascites tumor: substrate specificity and inhibition by bisubstrate analogs.
Cheng, N; Kemp, WE; Payne, RC; Traut, TW, 1986
)
2.09

Actions

Both uridine and inosine inhibit [3H]adenosine uptake. Uridine does not suppress glucose-regulated protein synthesis that has been induced by glycosylation inhibitors, calcium chelation, or anoxia.

ExcerptReferenceRelevance
"Both uridine and inosine inhibit [3H]adenosine uptake, suggesting that the Na-dependent transporter has broad substrate specificity for both purine and pyrimidine ribonucleosides."( Sodium-adenosine cotransport in brush-border membranes from rabbit ileum.
Betcher, SL; Dobbins, JW; Forrest, JN; Knickelbein, RG, 1990
)
0.73
"Uridine does not suppress glucose-regulated protein synthesis that has been induced by glycosylation inhibitors, calcium chelation, or anoxia."( Nucleoside restoration of heat resistance and suppression of glucose-regulated protein synthesis by glucose-deprived L929 cells.
Gao, JP; Kasambalides, EJ; Lanks, KW, 1988
)
1

Treatment

Uridine treatment at the dose of 500 mg/kg significantly decreased as apoptosis determined by Caspase-3/Actin ratio and exhibited significant anti-oxidant effects. Uridine triacetate treatment within 96 hours of administration is associated with survival.

ExcerptReferenceRelevance
"Uridine treatment at the dose of 500 mg/kg significantly decreased as apoptosis determined by Caspase-3/Actin ratio and exhibited significant anti-oxidant effects as determined by decreased levels of MPO and MDA as well as increased levels of SOD, GPx, and CAT compared to controls. "( Anti-Apoptotic and Anti-Oxidant Effects of Systemic Uridine Treatment in an Experimental Model of Sciatic Nerve Injury.
Bekar, A; Cakir, A; Cansev, M; Kafa, IM; Khezri, MK; Koc, C; Levent, P; Salman, B; Turkkan, A, 2021
)
2.31
"Uridine triacetate treatment within 96 hours of administration is associated with survival."( 5-Fluorouracil and Capecitabine: Assessment and Treatment of Uncommon Early-Onset Severe Toxicities Associated With Administration.
Brutcher, E; Christensen, D; Hennessey Smith, M; Koutlas, JB; Sellers, JB; Thompson, J; Timmons, T, 2018
)
1.2
"Uridine treatment also increased intracellular levels of cytidine triphosphate, which suggests that uridine may affect neurite outgrowth by enhancing phosphatidylcholine synthesis."( Uridine enhances neurite outgrowth in nerve growth factor-differentiated PC12 [corrected].
Benedictus, R; Guez, DH; Pooler, AM; Wurtman, RJ, 2005
)
2.49
"Deazauridine treatment of L1210 cells in culture stimulated the uptake of deoxycytidine-3H into DNA while inhibiting the uptake of 3H-labeled deoxyuridine, thymidine, deoxyadenosine, and deoxyguanosine."( The mechanism of action of 3-deazauridine in tumor cells sensitive and resistant to arabinosylcytosine.
Brockman, RW; Nelson, JA; Rose, LM; Schabel, FM; Shaddix, SC; Williams, M, 1975
)
0.99
"Treatment with uridine reduces apoptosis and oxidation in a rat model of sciatic nerve injury dose-dependently. "( Anti-Apoptotic and Anti-Oxidant Effects of Systemic Uridine Treatment in an Experimental Model of Sciatic Nerve Injury.
Bekar, A; Cakir, A; Cansev, M; Kafa, IM; Khezri, MK; Koc, C; Levent, P; Salman, B; Turkkan, A, 2021
)
1.22
"Treatment with uridine triacetate was arranged in the emergency department."( The successful treatment of 5-fluorouracil (5-FU) overdose in a patient with malignancy and HIV/AIDS with uridine triacetate.
Geller, RJ; Morgan, BW; Santos, C, 2017
)
1.01
"Treating uridine as a product of UTP degradation and hypoxanthine as a degradation product of ATP, we assessed the concentration of uridine and hypoxanthine in the blood of children with newly diagnosed type 1 diabetes. "( Uridine correlates with the concentration of fructosamine and HbA1c in children with type 1 diabetes.
Dudzinska, W, 2011
)
2.23
"Treatment with uridine alone did not protect from FUra toxicity at 200, 300, and 400 mg/kg as all of the mice died."( Potent combination therapy for human breast tumors with high doses of 5-fluorouracil: remission and lack of host toxicity.
Al Safarjalani, ON; el Kouni, MH; Naguib, FN; Rais, R, 2012
)
0.72
"Treatment with uridine alone did not protect from FUra toxicity at the dose of 200 mg/kg as all mice died."( Modulation of 5-fluorouracil host-toxicity and chemotherapeutic efficacy against human colon tumors by 5-(Phenylthio)acyclouridine, a uridine phosphorylase inhibitor.
Al Safarjalani, ON; el Kouni, MH; Naguib, FN; Rais, R; Schinazi, RF; Shi, J, 2006
)
0.88
"Pretreatment with uridine phosphorylase prior to administration of [3H]uridine produced a marked (65-92%) but incomplete inhibition of salvage of uridine in all tissues examined."( Salvage of uridine in the mouse. Effect of uridine phosphorylase pretreatment.
Henderson, JF; Moyer, JD, 1985
)
0.98

Toxicity

beta-D-Uridine protected human granulocyte-macrophage lineage cells against the toxic effects of 3'-azido-3. The combination of PTAU plus uridine can provide a better substitute for the large doses of uridine necessary to rescue or protect from FUra host-toxicities.

ExcerptReferenceRelevance
" This drug combination was severely toxic when 3-deazauridine was administered 2 to 8 hr prior to 1-beta-D-arabinofuranosylcytosine; most mice treated in this way died within 3 days of the last treatment."( Drug sequence-dependent toxicity and small bowel mucosal injury in mice treated with low doses of 3-deazauridine and 1-beta-D-arabinofuranosylcytosine.
Jakobs, ES; Lauzon, GJ; Paterson, AR; Weinstein, WM, 1979
)
0.72
" FdUrd, in particular, had a very minor effect on rRNA production even at very toxic drug concentrations."( Correlation between ribosomal RNA production and RNA-directed fluoropyrimidine cytotoxicity.
Armstrong, RD; Cadman, EC; Takimoto, CH; Tan, YY, 1987
)
0.27
" 3N-3DU exhibited comparable toxicity to ribavirin in KB cells, was 4-fold less toxic in WISH cells and 4-fold more toxic in LLC-MK2 cells."( Antiviral and cytotoxicity evaluation of 3-nitro-3-deazauridine.
Allen, LB; Cook, PD; Holland, CS; Kehoe, MJ; McNamara, DJ; Teepe, AG, 1989
)
0.52
" Lidoflazine had fewer adverse effects."( Modulation of 5-fluorouracil and 5-fluorouridine toxicity by membrane transport inhibitors in normal tissues of rats with liver adenocarcinoma.
Christensson, PI; el Hag, IA; Erichsen, C; Jakobsson, B; Jönsson, PE; Stenram, U,
)
0.4
" All three tumor cell lines were more sensitive to OHUrd than were the FeInt cells, whereas 5-FU was more toxic to the latter."( Selective cytotoxicity of 5-hydroxyuridine for human colon adenocarcinoma cells.
Giovanella, BC; Lockshin, A; Mendoza, JT; Stehlin, JS; Warneke, C,
)
0.41
" At concentrations of up to 50 microM no natural 2'-deoxynucleosides, including thymidine, were able to reverse the toxic effects of AZT."( Uridine reverses the toxicity of 3'-azido-3'-deoxythymidine in normal human granulocyte-macrophage progenitor cells in vitro without impairment of antiretroviral activity.
Carlisle, R; Schinazi, RF; Sommadossi, JP; Zhou, Z, 1988
)
1.72
"The toxic properties of human recombinant tumor necrosis factor (TNF) were investigated in mice made hypersensitive to endotoxin by treatment with D-galactosamine."( Lethal toxicity of lipopolysaccharide and tumor necrosis factor in normal and D-galactosamine-treated mice.
Freudenberg, MA; Galanos, C; Lehmann, V, 1987
)
0.27
" Our results suggest that the dose-related stimulatory, permeabilizing, and toxic effects of AmB most probably have distinct mechanisms of action and may be independent of one another."( Stimulatory, permeabilizing, and toxic effects of amphotericin B on L cells.
Brajtburg, J; Elberg, S; Kobayashi, GS; Medoff, G; Medoff, J; Schlessinger, D, 1984
)
0.27
" This side effect was also seen after administration of uridine (10 g/sq m) during combination with 5-fluorouracil."( Phase I and pharmacokinetic studies of high-dose uridine intended for rescue from 5-fluorouracil toxicity.
Gall, H; Kraal, I; Lankelma, J; Leyva, A; Peters, GJ; Pinedo, HM; van Groeningen, CJ, 1984
)
0.77
" It was observed that 5-Med-Cyd exerts its effects via deamination to thymidine, which is particularly toxic to human promyelocytic (HL-60) and T-cell (JM) leukemia cell lines in vitro."( Reversal of deamination-related cytotoxicity of 5-methyl-2'-deoxycytidine by tetrahydrouridine in human leukemia cells.
Jekunen, A; Vilpo, JA, 1984
)
0.49
" The test compounds, which included alcohols, ethers, esters, ketones, amides, acids and a detergent, inhibited uridine uptake at concentrations lower than those required to kill the cells; thus uridine uptake inhibition is a more sensitive indicator of toxic action than is cell lethality."( Uridine uptake inhibition as a cytotoxicity test: correlations with the Draize test.
Sathe, S; Shopsis, C, 1984
)
1.92
"The toxic side effects of certain antimicrobial agents are probably related to their membrane damaging properties."( Cultured human fibroblasts as a model for evaluation of potential in vivo toxicity of membrane damaging antibiotics.
Möllby, R; Thelestam, M, 1980
)
0.26
" 4-OH-IF and 4-OH-CP were significantly more toxic than the parent drugs."( Toxicity of ifosfamide, cyclophosphamide and their metabolites in renal tubular cells in culture.
Ansorge, S; Brandis, M; Mohrmann, M; Schmich, U; Schönfeld, B, 1994
)
0.29
" Results suggest that the components that leach out of the tested materials do so at different rates and have prolonged toxic effects on cells."( Cytotoxicity of eluates from light-polymerized denture base resins.
Knoernschild, KL; Lefebvre, CA; Schuster, GS, 1994
)
0.29
"The model of toxic liver injury was used to examine the role of manganese superoxide dismutase (MnSOD) expression in cellular resistance to tumor necrosis factor (TNF)-alpha toxicity."( Induction of MnSOD gene expression in a hepatic model of TNF-alpha toxicity does not result in increased protein.
Compton, A; Czaja, MJ; Oberley, LW; Ridnour, L; Schilsky, ML; Schmiedeberg, P; Xu, Y, 1994
)
0.29
" Comparing the rescue effect of two dose schedules of uridine, both high dose (2 x 3500 mg/kg) or repeated lower doses of uridine (7 x 800 mg/kg) resulted in a similar protection from the gastrointestinal side effect of 5-FU."( Influence of uridine treatment in mice on the protection of gastrointestinal toxicity caused by 5-fluorouracil.
Bagrij, T; Gyergyay, F; Kiss, E; Kralovanszky, J; Peters, GJ,
)
0.75
") is equally toxic to both wild-type and adenosine-kinase-deficient BHK cells at concentrations up to 100 microM; at higher concentrations, wild-type cells are more sensitive, as are cells over-expressing adenosine kinase."( The bis(adenosin-N6-yl) alkanes, a family of potential dinucleoside polyphosphate analogue precursors. Mechanism of growth inhibition and suppression of adenosine toxicity in lymphoid cells.
Chen, H; McLennan, AG, 1993
)
0.29
"Selective protection of the normal host tissues from the toxic effects of anticancer agents would allow the use of higher, probably more effective, doses of the drugs."( Biochemical consequences of 5-fluorouracil gastrointestinal toxicity in rats; effect of high-dose uridine.
Bagrij, T; Kerpel-Fronius, S; Kiss, E; Kralovanszky, J; Peters, GJ; Prajda, N, 1993
)
0.5
"beta-D-Uridine protected human granulocyte-macrophage lineage cells in both semi-solid (granulocyte-macrophage colony-forming units, CFU-GM) and liquid cultures against the toxic effects of 3'-azido-3'-deoxythymidine (AZT), 3'-fluoro-3'-deoxythymidine (FLT) and a combination of AZT and FLT, without impairment of the activities of these respective drugs against human immunodeficiency virus (HIV) replication."( Selective protection of toxicity of 2',3'-dideoxypyrimidine nucleoside analogs by beta-D-uridine in human granulocyte-macrophage progenitor cells.
Faraj, A; Gosselin, G; Imbach, JL; Perigaud, C; Schinazi, RF; Sommadossi, JP; Xie, MY, 1996
)
0.97
" Our study suggests that liposome-encapsulated 5-FUR is not toxic to the retina even at doses of 1 mg."( Pharmacokinetics and retinal toxicity of intravitreal liposome-encapsulated 5-fluorouridine.
Casaroli, R; Corcostegui, B; Fonseca, MJ; García-Arumí, J; Isart, FR; Mateo, C; Pascual, R, 1997
)
0.52
"We investigated the relationship between the toxic effect of allopurinol and pyrimidine metabolism in mice."( Allopurinol induces renal toxicity by impairing pyrimidine metabolism in mice.
Horiuchi, H; Kaneko, H; Kasahara, Y; Komoriya, K; Nishimura, S; Ohta, T; Ota, M, 2000
)
0.31
" The present results suggest that the BBBA plus TAU combination can provide a better substitute for the massive doses of uridine required to achieve the high levels of uridine necessary to rescue or protect from FUra host toxicities without the toxic side-effects associated with such doses of uridine."( Modulation of 5-fluorouracil host toxicity by 5-(benzyloxybenzyl)barbituric acid acyclonucleoside, a uridine phosphorylase inhibitor, and 2',3',5'-tri-O-acetyluridine, a prodrug of uridine.
Al Safarjalani, ON; Ashour, OM; el Kouni, MH; Naguib, FN; Panzica, RP, 2000
)
0.73
" Uridine uptake was always inhibited at lower concentrations than those required in the neutral red assay, suggesting that the uridine uptake assay is a more sensitive indicator of toxic action than the neutral red inclusion."( Uridine uptake inhibition as a cytotoxicity test for a human hepatoma cell line (HepG2 cells): comparison with the neutral red assay.
Chagnon, M; Lhuguenot, J; Philippe, M; Valentin, I, 2001
)
2.66
" There are no toxic effects of 5-fodUrd on cells defective in thymidine kinase or thymidylate synthetase, suggesting that the toxicity may be caused by 5-fodUrd phosphorylation and subsequent inhibition of thymidylate synthetase."( 5-Formyluracil and its nucleoside derivatives confer toxicity and mutagenicity to mammalian cells by interfering with normal RNA and DNA metabolism.
Bjelland, S; Klungland, A; Matsuda, A; Paulsen, R; Rolseth, V; Seeberg, E; Ueno, Y; Wiik, P; Yamada, Y, 2001
)
0.31
" To evaluate its sensitivity, we compared the IC(50) values obtained with new and original protocol for each eight toxic compounds."( Uridine uptake inhibition assay: an automated micromethod for the screening of cytotoxicity.
Chagnon, MC; Laignelet, L; Lhuguenot, JC; Valentin-Severin, I, 2002
)
1.76
" Uridine fully abrogated the adverse effects of zalcitabine on hepatocyte proliferation and normalized lactate synthesis, intracellular lipids and COX II levels by adjusting mtDNA levels to about 65% of NRTI-unexposed control cells."( Uridine abrogates mitochondrial toxicity related to nucleoside analogue reverse transcriptase inhibitors in HepG2 cells.
Koch, EC; Olschewski, M; Schneider, J; Setzer, B; Venhoff, N; Walker, UA, 2003
)
2.67
" Motor scores, as measured by the UPDRS motor subscale, showed mild improvement, which demonstrates that galantamine has no adverse effect on parkinsonian symptoms."( Efficacy and safety of galantamine in patients with dementia with Lewy bodies: a 12-week interim analysis.
Bednarczyk, EM; Edwards, KR; Farlow, M; Hershey, L; Johnson, S; Lichter, D; Wray, L, 2004
)
0.32
" The percent of subjects experiencing adverse events was similar between the denufosol and placebo groups."( Safety and tolerability of denufosol tetrasodium inhalation solution, a novel P2Y2 receptor agonist: results of a phase 1/phase 2 multicenter study in mild to moderate cystic fibrosis.
Daines, C; Deterding, R; Engels, J; Gibson, R; Gorden, J; Lavange, L; Marshall, B; Mathews, D; Milgram, L; Milla, C; Ramsey, B; Retsch-Bogart, G; Schaberg, A; Williams, J; Zeitlin, PL, 2005
)
0.33
" The current safety data justify the closely monitored use of uridine in individuals who suffer from mt toxicity but who cannot be switched to less toxic NRTIs."( Uridine in the prevention and treatment of NRTI-related mitochondrial toxicity.
Venhoff, N; Walker, UA, 2005
)
2.01
" We assessed whether uridine can abrogate the adverse effects of NRTIs on adipocyte functions."( Uridine abrogates the adverse effects of antiretroviral pyrimidine analogues on adipose cell functions.
Auclair, M; Capeau, J; Caron, M; Kornprobst, M; Lebrecht, D; Walker, UA, 2006
)
2.1
" Uridine (200 microM) had no intrinsic effect, but prevented all adverse effects of d4T, ZDV and ddC on adipocyte morphology, lipid staining, apoptosis, mtDNA depletion (partial prevention with ZDV), mitochondrial mass and membrane potential."( Uridine abrogates the adverse effects of antiretroviral pyrimidine analogues on adipose cell functions.
Auclair, M; Capeau, J; Caron, M; Kornprobst, M; Lebrecht, D; Walker, UA, 2006
)
2.69
"Uridine supplementation protects adipocytes from the adverse effects of d4T, ZDV and ddC on lipid accumulation, cell survival and mitochondrial functions, suggesting that the toxic effects could be linked to intracellular depletion of uridine or its metabolites."( Uridine abrogates the adverse effects of antiretroviral pyrimidine analogues on adipose cell functions.
Auclair, M; Capeau, J; Caron, M; Kornprobst, M; Lebrecht, D; Walker, UA, 2006
)
3.22
" Therefore, the combination of PTAU plus uridine can provide a better substitute for the large doses of uridine necessary to rescue or protect from FUra host-toxicities, without the toxic side-effects associated with such doses of uridine."( Modulation of 5-fluorouracil host-toxicity and chemotherapeutic efficacy against human colon tumors by 5-(Phenylthio)acyclouridine, a uridine phosphorylase inhibitor.
Al Safarjalani, ON; el Kouni, MH; Naguib, FN; Rais, R; Schinazi, RF; Shi, J, 2006
)
0.81
" The most common adverse event was cough (52% of placebo patients and 47% of denufosol patients)."( Phase 2 randomized safety and efficacy trial of nebulized denufosol tetrasodium in cystic fibrosis.
Brody, AS; Coquillette, SJ; Deterding, RR; Engels, JM; Lavange, LM; Mathews, DW; Millard, SP; Ramsey, BW, 2007
)
0.34
"Denufosol administered three times daily for 28 days appeared to be safe and well tolerated in this population with mild cystic fibrosis and provided preliminary evidence of potential benefit in lung function."( Phase 2 randomized safety and efficacy trial of nebulized denufosol tetrasodium in cystic fibrosis.
Brody, AS; Coquillette, SJ; Deterding, RR; Engels, JM; Lavange, LM; Mathews, DW; Millard, SP; Ramsey, BW, 2007
)
0.34
" No adverse events were noted throughout the study."( Uridine supplementation in HIV lipoatrophy: pilot trial on safety and effect on mitochondrial indices.
Baron, E; Lebrecht, D; McComsey, GA; O'Riordan, M; Setzer, B; Walker, UA, 2008
)
1.79
" These novel data highlight the applicability of NMR-based metabonomics in elucidating multicompartmental metabolic consequences of toxicity and toxic salvage."( The mechanism of galactosamine toxicity revisited; a metabonomic study.
Clayton, TA; Coen, M; Holmes, E; Hong, YS; Lindon, JC; Nicholson, JK; Pearce, JT; Reily, MD; Robertson, DG; Rohde, CM, 2007
)
0.34
" Mitocnol attenuated or normalized all myocardial pathology when given with both NRTI, but by itself had no intrinsic effects and no apparent adverse effects."( Role of pyrimidine depletion in the mitochondrial cardiotoxicity of nucleoside analogue reverse transcriptase inhibitors.
Balcarek, K; Beauvoit, B; Bonnet, J; Deveaud, C; Kirschner, J; Lebrecht, D; Venhoff, AC; Venhoff, N; Walker, UA, 2010
)
0.36
" This procedure provides the following advantages: 1) it uses common, affordable mammalian cells (HeLa cells, WI38VA13 cells, human dermal fibroblasts, or Chinese hamster ovary cells) rather than genetically modified microorganisms; 2) it can be completed within approximately 8 hr after the cells are prepared because RNA polymerase responses during TC-NER are faster than other DNA damage responses (replication, recombination, and apoptosis); and 3) it is safe because it uses non-radioactive bromouridine and antibodies to detect RNA synthesis on undamaged transcribed DNA strands."( A method for detecting genetic toxicity using the RNA synthesis response to DNA damage.
Iwai, S; Kuraoka, I; Morita, Y, 2011
)
0.53
" Therefore, the combination of PTAU plus uridine can provide a better substitute for the massive doses of uridine necessary to rescue or protect from FUra host-toxicities, without the toxic side effects associated with such doses of uridine."( Potent combination therapy for human breast tumors with high doses of 5-fluorouracil: remission and lack of host toxicity.
Al Safarjalani, ON; el Kouni, MH; Naguib, FN; Rais, R, 2012
)
0.64
" Antiviral nucleosides are known to cause toxic mitochondrial side effects."( Zidovudine induces downregulation of mitochondrial deoxynucleoside kinases: implications for mitochondrial toxicity of antiviral nucleoside analogs.
Eriksson, S; Sun, R; Wang, L, 2014
)
0.4
" It was shown that the dialdehyde derivatives of uridine, 1-β-D-eritrofuranozyl uracil and 3'-O-β-D-ribofuranosyl-2'-deoxythymidine, in contrast to their unoxidized counterparts, exert marked toxic effect on SKOV-3 cells."( [The selective toxic effect of dialdehyde derivatives of the pyrimidine nucleosides on human tumor cells].
Drenichev, MS; Efremova, AS; Mihaylov, SN; Myasoedov, NF; Posypanova, GA; Shram, SI,
)
0.39
"5 weeks (range 3-4 weeks), indicating that Vistogard might be able to delay 5-FU toxicity despite higher doses than standard bolus dose of 5-FU used in gastrointestinal malignancies and the appearance of a potentially less toxic adverse effect of 5-FU at an unusual site (cutaneous) in one patient."( Benefit of uridine triacetate (Vistogard) in rescuing severe 5-fluorouracil toxicity in patients with dihydropyrimidine dehydrogenase (DPYD) deficiency.
Diasio, RB; Saif, MW, 2016
)
0.82
" Uridine triacetate delivers high concentrations of uridine, which competes with toxic 5-FU metabolites."( Emergency use of uridine triacetate for the prevention and treatment of life-threatening 5-fluorouracil and capecitabine toxicity.
Bamat, MK; Cartwright, TH; El-Rayes, BF; Fakih, MG; King, TR; Ma, WW; Posey, JA; Saif, MW; von Borstel, RW, 2017
)
1.7
" Adverse reactions in patients receiving uridine triacetate included vomiting (8."( Emergency use of uridine triacetate for the prevention and treatment of life-threatening 5-fluorouracil and capecitabine toxicity.
Bamat, MK; Cartwright, TH; El-Rayes, BF; Fakih, MG; King, TR; Ma, WW; Posey, JA; Saif, MW; von Borstel, RW, 2017
)
1.06
"In these studies, uridine triacetate was a safe and effective lifesaving antidote for capecitabine and 5-FU overexposure, and it facilitated the rapid resumption of chemotherapy."( Emergency use of uridine triacetate for the prevention and treatment of life-threatening 5-fluorouracil and capecitabine toxicity.
Bamat, MK; Cartwright, TH; El-Rayes, BF; Fakih, MG; King, TR; Ma, WW; Posey, JA; Saif, MW; von Borstel, RW, 2017
)
1.13
" The most common adverse events were headache (143 [22%] of 664), fatigue (129 [19%] of 664), and nausea (83 [13%] of 664)."( Safety and efficacy of a fixed-dose combination regimen of grazoprevir, ruzasvir, and uprifosbuvir with or without ribavirin in participants with and without cirrhosis with chronic hepatitis C virus genotype 1, 2, or 3 infection (C-CREST-1 and C-CREST-2,
Almasio, PL; Barr, E; Bruno, S; Buti, M; Butterton, JR; Dutko, FJ; Fernsler, D; Gao, W; Grandhi, A; Hassanein, TI; Huang, HC; Jancoriene, L; Lawitz, E; Li, JJ; Liu, H; Muellhaupt, B; Nguyen, BT; Pearlman, B; Plank, RM; Robertson, MN; Ruane, PJ; Shepherd, A; Su, FH; Tannenbaum, B; Vierling, JM; Wahl, J; Wan, S; Yeh, WW; Yoshida, EM, 2017
)
0.46
" Overall, the most common adverse events were headache (55 [23%] of 240), fatigue (47 [20%] of 240), and nausea (32 [13%] of 240)."( Safety and efficacy of an 8-week regimen of grazoprevir plus ruzasvir plus uprifosbuvir compared with grazoprevir plus elbasvir plus uprifosbuvir in participants without cirrhosis infected with hepatitis C virus genotypes 1, 2, or 3 (C-CREST-1 and C-CREST
Agarwal, K; Barr, E; Ben-Ari, Z; Butterton, JR; Chen, HL; Dutko, FJ; Esteban, R; Fernsler, D; Fitzgerald, B; Foster, GR; Gane, EJ; Gao, W; Gerstoft, J; Grandhi, A; Huang, HC; Laursen, AL; Li, JJ; Liu, H; Nguyen, BT; Pianko, S; Plank, RM; Roberts, SK; Robertson, MN; Su, FH; Thompson, AJ; Wahl, J; Wan, S; Yeh, WW; Zeng, Z; Zeuzem, S; Zuckerman, E, 2017
)
0.46
" This review summarizes the current state of knowledge of FIC with special regard to proposed pathogenetic models (coronary vasospasm, endothelium and cardiomyocytes damage, toxic metabolites, dihydropyrimidine dehydrogenase deficiency); risk and predictive factors; efficacy and usefulness in detection of laboratory markers, electrocardiographic changes and cardiac imaging; and specific treatment, including a novel agent, uridine triacetate."( Fluoropyrimidine-induced cardiotoxicity.
Aglietta, M; Bonzano, A; Cagnazzo, C; Depetris, I; Filippi, R; Leone, F; Marino, D, 2018
)
0.65
" Adverse events (AEs) were reported by 61."( Efficacy and safety of a two-drug direct-acting antiviral agent regimen ruzasvir 180 mg and uprifosbuvir 450 mg for 12 weeks in adults with chronic hepatitis C virus genotype 1, 2, 3, 4, 5 or 6.
Barr, E; Burnevich, E; Buti, M; Feld, JJ; Foster, GR; Gane, E; Hanna, GJ; Jackson, B; Katchman, H; Klopfer, S; Lahser, F; Lawitz, E; Platt, HL; Rabinovitz, M; Robertson, MN; Shaughnessy, M; Tomasiewicz, K; Yeh, WW, 2019
)
0.51

Pharmacokinetics

The uridine analog 3-deazauridine has been given to 19 patients in a phase I and pharmacokinetic study. Uridine plasma decay curves were biphasic with a terminal half-life of 118 min.

ExcerptReferenceRelevance
" This results in a decrease in ara-C catabolism and prolongs the plasma half-life of ara-C."( Modulation of the metabolism and pharmacokinetics of 1-beta-D-arabinofuranosylcytosine by 1-beta-D-arabinofuranosyluracil in leukemic mice.
Capizzi, RL; Chandrasekaran, B; Dimling, J; Kute, TE; Morgan, T, 1989
)
0.28
" Furthermore the differing levels of 5-FU metabolites in normal and malignant tissue could not be correlated with the pharmacokinetic parameters studied."( The relationship between plasma pharmacokinetics and tissue metabolites of 5-fluorouracil (5-FU) in patients with colorectal cancer.
Chisholm, EM; Finan, PJ; Giles, GR; Woodhouse, L, 1987
)
0.27
"Described are some pharmacokinetic parameters for 5-fluorouridine, a potentially useful intermediate metabolite of 5-fluorouracil (5-FU), following subconjunctival and intravitreal injection in the pigmented rabbit."( Uptake and clearance of 5-fluorouridine following subconjunctival and intravitreal injection.
Blumenkranz, MS; Hartzer, M; Hernandez, E; Huang, DS, 1988
)
0.8
" administration followed first-order kinetics with a half-life of approximately 36 min."( Benzylacyclouridine. Pharmacokinetics, metabolism and biochemical effects in mice.
Darnowski, JW; Handschumacher, RE, 1988
)
0.65
"62 min and a terminal half-life of 17."( Uridine pharmacokinetics in cancer patients.
Abramson, I; Chan, TC; Howell, SB; Markman, M; Pfeifle, CE; Taetle, R, 1988
)
1.72
"A clinical and pharmacokinetic investigation of prolonged administration of high-dose uridine was performed in seven patients with advanced-stage cancer."( Clinical and pharmacokinetic studies of prolonged administration of high-dose uridine intended for rescue from 5-FU toxicity.
Kraal, I; Leyva, A; Peters, GJ; Pinedo, HM; van Groeningen, CJ, 1986
)
0.72
" Uridine plasma decay curves were biphasic with a terminal half-life of 118 min."( Phase I and pharmacokinetic studies of high-dose uridine intended for rescue from 5-fluorouracil toxicity.
Gall, H; Kraal, I; Lankelma, J; Leyva, A; Peters, GJ; Pinedo, HM; van Groeningen, CJ, 1984
)
1.43
"The uridine analog 3-deazauridine has been given to 19 patients in a phase I and pharmacokinetic study."( Phase I trial and pharmacokinetics of a daily x 5 schedule of 3-deazauridine.
Bruno, S; Creaven, PJ; Henderson, ES; Mittelman, A; Priore, RL; Rustum, YM; Solomon, JK, 1982
)
1.06
" In addition, uridine pharmacokinetics were associated with a time-dependent relationship as evidenced by an increased total plasma clearance, renal clearance and volume of distribution, resulting in a substantial decrease in uridine peak concentration with time."( Effects of 5-benzylacyclouridine, an inhibitor of uridine phosphorylase, on the pharmacokinetics of uridine in rhesus monkeys: implications for chemotherapy.
Anderson, DC; Cretton, EM; el Kouni, MH; Kidd, LB; McClure, HM; Sommadossi, JP, 1995
)
0.96
" Liposome encapsulation of these antiproliferative drugs may extend the intravitreal half-life and increase their efficacy."( Pharmacokinetics and retinal toxicity of intravitreal liposome-encapsulated 5-fluorouridine.
Casaroli, R; Corcostegui, B; Fonseca, MJ; García-Arumí, J; Isart, FR; Mateo, C; Pascual, R, 1997
)
0.52
"The current study evaluated the pharmacokinetic behavior of intravitreally injected 5-fluorouridine (5-FUR), free and encapsulated in liposomes, either conventionally or coated with collagen into 25 New Zealand rabbits."( Pharmacokinetics and retinal toxicity of intravitreal liposome-encapsulated 5-fluorouridine.
Casaroli, R; Corcostegui, B; Fonseca, MJ; García-Arumí, J; Isart, FR; Mateo, C; Pascual, R, 1997
)
0.74
"The half-life of free 5-FUR after liposome injection into the vitreous cavity was 18."( Pharmacokinetics and retinal toxicity of intravitreal liposome-encapsulated 5-fluorouridine.
Casaroli, R; Corcostegui, B; Fonseca, MJ; García-Arumí, J; Isart, FR; Mateo, C; Pascual, R, 1997
)
0.52
" The plasma levels of PTAU as well as those of uridine and its catabolite uracil were measured by HPLC, and pharmacokinetic analysis was performed."( Modulation of the pharmacokinetics of endogenous plasma uridine by 5-(phenylthio)acyclouridine, a uridine phosphorylase inhibitor: implications for chemotherapy.
Al Safarjalani, ON; el Kouni, MH; Goudgaon, NM; Naguib, FN; Schinazi, RF; Zhou, XJ, 2001
)
0.81
" The purpose of this study was to investigate the pharmacokinetic properties of doxifluridine and its two major metabolites, 5-FU, and 5-fluorouridine (5-FUrd), in beagle dogs following a single oral administration of 200 mg doxifluridine capsule (Furtulon(®))."( Pharmacokinetic analysis of doxifluridine and its metabolites, 5-fluorouracil and 5-fluorouridine, after oral administration in beagle dogs.
Baek, IH; Kim, MS; Kwon, KI; Lee, BY, 2013
)
0.89
" Pharmacokinetics and safety assessments were performed, and pharmacokinetic parameters were calculated using non-compartmental methods and summarized using descriptive statistics and compared statistically by geometric least-squares mean ratios and 90% confidence intervals."( Pharmacokinetics and Safety of Velpatasvir and Sofosbuvir/Velpatasvir in Subjects with Hepatic Impairment.
Brainard, DM; Curtis, C; Lasseter, K; Lawitz, E; Ling, KHJ; Marbury, T; Mathias, A; Mogalian, E; Moorehead, L; Murray, B; Osinusi, A; Perry, R, 2018
)
0.48
"The purpose of this study was to investigate the safety, tolerability, and pharmacokinetic profile of sofosbuvir and its metabolites after a single dose of sofosbuvir 400mg and once daily dosing of sofosbuvir 400mg for 7days in healthy Chinese subjects."( Pharmacokinetics, Safety, and Tolerability of the Direct-acting Hepatitis C Antiviral Sofosbuvir in HealthyChineseSubjects.
Brainard, DM; Chen, G; Chen, H; Ding, Y; Li, X; Massetto, B; Niu, J; Shen, G; Zhang, H; Zhu, X, 2018
)
0.48
" The pharmacokinetic properties of sofosbuvir, GS-556500, and GS-311007 were found to be broadly similar in healthy Chinese subjects compared with non-Chinese subjects in previous sofosbuvir studies."( Pharmacokinetics, Safety, and Tolerability of the Direct-acting Hepatitis C Antiviral Sofosbuvir in HealthyChineseSubjects.
Brainard, DM; Chen, G; Chen, H; Ding, Y; Li, X; Massetto, B; Niu, J; Shen, G; Zhang, H; Zhu, X, 2018
)
0.48
"AL-335 was well tolerated when administered as single and multiple doses, with an acceptable pharmacokinetic profile."( Safety, tolerability, and pharmacokinetics of AL-335 in healthy volunteers and hepatitis C virus-infected subjects.
Astruc, B; Beigelman, L; Berliba, E; Blatt, LM; Chanda, S; Fry, J; Kakuda, TN; Khorlin, N; McClure, MW; Patat, A; Streinu-Cercel, A; Tsertsvadze, T; Vijgen, L; Vuong, J; Westland, C; Zhang, Q, 2018
)
0.48
"Limited data exist on the pharmacokinetic profile of novel direct-acting antivirals in kidney transplant recipients."( Pharmacokinetics of Daclatasvir, Sofosbuvir, and GS-331007 in a Prospective Cohort of Hepatitis C Virus-Positive Kidney Transplant Recipients.
Algharably, E; Budde, K; Duerr, M; Glander, P; Halleck, F; Hoffmann, F; Jaeger, C; Kreutz, R; Lisec, J; Schrezenmeier, E; Schrezenmeier, J, 2019
)
0.51
" This study provides the rationale for future studies investigating the pharmacokinetic profile of sofosbuvir-based HCV treatment in kidney transplant recipients with an eGFR <30 mL/min."( Pharmacokinetics of Daclatasvir, Sofosbuvir, and GS-331007 in a Prospective Cohort of Hepatitis C Virus-Positive Kidney Transplant Recipients.
Algharably, E; Budde, K; Duerr, M; Glander, P; Halleck, F; Hoffmann, F; Jaeger, C; Kreutz, R; Lisec, J; Schrezenmeier, E; Schrezenmeier, J, 2019
)
0.51
" This analysis evaluated the drug-drug interaction (DDI) following co-administration of ertugliflozin with the UGT inhibitor mefenamic acid (MFA) using physiologically-based pharmacokinetic (PBPK) modeling."( Physiologically-Based Pharmacokinetic Modeling of the Drug-Drug Interaction of the UGT Substrate Ertugliflozin Following Co-Administration with the UGT Inhibitor Mefenamic Acid.
Callegari, E; Goosen, TC; Lin, J; Sahasrabudhe, V; Tse, S, 2021
)
0.62

Compound-Compound Interactions

ExcerptReferenceRelevance
"2 mg/kg/day when administered in combination with a sub-effective dose of human recombinant interferon-beta."( Inhibition of simian varicella virus infection of monkeys by 1-(2-deoxy-2- fluoro-1-beta-D-arabinofuranosyl)-5-ethyluracil (FEAU) and synergistic effects of combination with human recombinant interferon-beta.
Chou, TC; Fox, JJ; Gloff, CA; Soike, KF; Watanabe, KA, 1990
)
0.28
"We have evaluated the effect of nucleoside related compounds on a murine tumor given with local radiotherapy and on the survival rate following whole body irradiation."( [The modification of radiation effect by nucleoside related compounds on a murine tumor given with local radiotherapy and on survival following whole body irradiation].
Sougawa, M; Tanaka, Y, 1989
)
0.28
"In the search for cytokines whose antiproliferative action could be enhanced by combination with dipyridamole, 2,6-bis(diethanolamino)-4,8-dipiperidinopyrimido[5,4-d]pyrim idine, the combination of tumor necrosis factor-alpha (TNF-alpha) with this agent was evaluated in various human tumor cell lines."( Dipyridamole combined with tumor necrosis factor-alpha enhances inhibition of proliferation in human tumor cell lines.
Kojima, T; Sekiya, S; Sugano, I; Suzuki, N; Takakubo, Y; Yamamori, H, 1995
)
0.29
" Hence administering omega-3 polyunsaturated fatty acids can enhance synaptic membrane levels in gerbils, and may do so in patients with neurodegenerative diseases, especially when given with a uridine source, while the omega-6 polyunsaturated fatty acid arachidonic acid is ineffective."( Chronic administration of docosahexaenoic acid or eicosapentaenoic acid, but not arachidonic acid, alone or in combination with uridine, increases brain phosphatide and synaptic protein levels in gerbils.
Cansev, M; Wurtman, RJ, 2007
)
0.73
"A simple, fast and inexpensive method based on dispersive solid phase extraction (DSPE) combined with LC-MS was developed for simultaneous determination of 7 nucleosides and nucleobases (i."( Determination of the nucleosides and nucleobases in Tuber samples by dispersive solid-phase extraction combined with liquid chromatography-mass spectrometry.
Li, HM; Li, YY; Liu, P; Tang, YJ; Wan, DJ, 2011
)
0.37
" When combined with GSK983, CPU resulted in large drops in cellular UTP and CTP pools."( Enhancing the Antiviral Efficacy of RNA-Dependent RNA Polymerase Inhibition by Combination with Modulators of Pyrimidine Metabolism.
Bassik, MC; Carette, JE; Fischer, CR; Gupta, A; Khosla, C; Liu, Q; Okesli-Armlovich, A; Qiao, W; Smith, M, 2020
)
0.56
" This analysis evaluated the drug-drug interaction (DDI) following co-administration of ertugliflozin with the UGT inhibitor mefenamic acid (MFA) using physiologically-based pharmacokinetic (PBPK) modeling."( Physiologically-Based Pharmacokinetic Modeling of the Drug-Drug Interaction of the UGT Substrate Ertugliflozin Following Co-Administration with the UGT Inhibitor Mefenamic Acid.
Callegari, E; Goosen, TC; Lin, J; Sahasrabudhe, V; Tse, S, 2021
)
0.62

Bioavailability

The purpose of this investigation was to evaluate the effectiveness of oral 5-(phenylselenenyl)-acyclouridine (PSAU) in increasing endogenous plasma uridine concentration. PSAU has 100% oral bioavailability and is a powerful enhancer of the bioavailability of oral uridine.

ExcerptReferenceRelevance
" The therapeutic advantage of combination chemotherapy may reside in the whole organism, reflecting increased bioavailability of drug, reduced dose-limiting toxicity or reduced impairment of host defenses; it may reside in the tumor cells, reflecting the multiple molecular mechanisms of interaction mentioned above."( Multiple basis of combination chemotherapy.
Grindey, GB; Mihich, E, 1977
)
0.26
" High amounts of uracil formed from uridine can interfere with the hepatic catabolism of 5-fluorouracil and thus increase its bioavailability and toxicity."( Uridine catabolism by the isolated perfused rat liver.
Gengenbacher, HM; Gerok, W; Holstege, A; Jehle, L, 1992
)
2
" Oral administration of uridine has also been studied, but bioavailability was low."( Modulation of fluorouracil toxicity with uridine.
Peters, GJ; Pinedo, HM; van Groeningen, CJ, 1992
)
0.86
" Recent clinical trials suggest that oral mesna has adequate bioavailability (roughly 50% by urinary thiol measurements) to prevent urotoxicity in high-dose ifosfamide regimens."( Chemoprotectants for cancer chemotherapy.
Dorr, RT, 1991
)
0.28
"Rectal bioavailability of Ara-C (serum AUC 4 h: 65 micrograms h-1 ml-1) administered in a suppository formulation containing tetrahydrouridine (a deamination inhibitor) and sodium salicylate (an adjuvant) to dogs was better than that from a suppository formulation without tetrahydrouridine (serum AUC 4 h: 18 micrograms h-1 ml-1)."( Enhanced serum concentrations of Ara-C using suppositories containing tetrahydrouridine as a deamination inhibitor of Ara-C.
Engle, KK; Higuchi, T; Liversidge, GG; Nishihata, T, 1986
)
0.7
" UR did not alter the Cl of dFUR, but reduced the absorption rate of dFUR from the gastrointestinal tract and significantly reduced the absolute oral bioavailability of dFUR from 55."( Effect of uridine coadministration on 5'-deoxy-5-fluorouridine disposition in rats.
Au, JL; Bramer, SL; Wientjes, MG, 1988
)
0.68
"We compared the bioavailability of uridine (Urd) (350 and 3500 mg/kg) administered either as a single SC injection or by gavage, in male CD8F1 mice."( Comparison of the bioavailability of uridine in mice after either oral or parenteral administration.
Cysyk, RL; Geffen, DB; Klubes, P, 1986
)
0.82
" However, the bioavailability of UK-21 given orally did not seem to be good."( Novel lowly immunosuppressive antitumor fluorouridine derivative, UK-21: antitumor activity and effect on humoral immune response in mice.
Kaku, Y; Kita, J; Koda, A; Maeda, D; Mori, H; Nagai, H; Nakayama, K, 1994
)
0.55
"This study in the rat established the effects that a broad-spectrum and poorly absorbed antibiotic, neomycin sulfate, had on the in vitro and in vivo hydrolysis of vicine and convicine by the intestinal microflora, and on vicine- and convicine-induced depletion of blood glutathione and the resulting toxicity."( Effect of neomycin on the hydrolysis and toxicity of vicine and convicine in rats.
Arbid, MS; Frohlich, AA; Madhyastha, MS; Marquardt, RR, 1993
)
0.29
" with BAU at 90 mg/kg, and a comparison of the AUC values showed an oral bioavailability of 70%."( Species-dependent differences in the biochemical effects and metabolism of 5-benzylacyclouridine.
Baccanari, DP; Chandrasurin, P; Davis, ST; Joyner, SS, 1993
)
0.51
"3), the enzyme responsible for uridine catabolism, and 2',3',5'-tri-O-acetyluridine (TAU), a prodrug of uridine, were used to investigate the possibility of improving the bioavailability of oral uridine in mice."( 5-(m-Benzyloxybenzyl)barbituric acid acyclonucleoside, a uridine phosphorylase inhibitor, and 2',3',5'-tri-O-acetyluridine, a prodrug of uridine, as modulators of plasma uridine concentration. Implications for chemotherapy.
Ashour, OM; el Kouni, MH; Naguib, FN, 1996
)
0.83
"6 g of PN401 as an oral suspension or 6 g given in tablet form resulted in high bioavailability of URD, with sustained plasma concentrations greater than 50 mumol/L."( Phase I trial of PN401, an oral prodrug of uridine, to prevent toxicity from fluorouracil in patients with advanced cancer.
Bertino, J; Kelsen, DP; Martin, D; O'Neil, J; Saltz, L; Schwartz, G; Sung, MT; von Borstel, R, 1997
)
0.56
"The purpose of this investigation was to evaluate the efficacy of oral 5-(phenylselenenyl)-acyclouridine (PSAU) in increasing endogenous plasma uridine concentration as well as its ability to improve the bioavailability of oral uridine."( Modulation of plasma uridine concentration by 5-(phenylselenenyl)acyclouridine, an inhibitor of uridine phosphorylase: relevance to chemotherapy.
Al Safarjalani, ON; Ashour, OM; el Kouni, MH; Goudgaon, NM; Naguib, FN; Schinazi, RF, 2000
)
0.84
"PSAU has an oral bioavailability of 100% and no PSAU metabolites were detected."( Modulation of plasma uridine concentration by 5-(phenylselenenyl)acyclouridine, an inhibitor of uridine phosphorylase: relevance to chemotherapy.
Al Safarjalani, ON; Ashour, OM; el Kouni, MH; Goudgaon, NM; Naguib, FN; Schinazi, RF, 2000
)
0.63
" Understanding the substrate selectivity of these transporters is critical in the development of therapeutic nucleoside analogs with optimal pharmacokinetic properties, including high oral bioavailability and tissue-specific distribution."( Electrophysiological analysis of the substrate selectivity of a sodium-coupled nucleoside transporter (rCNT1) expressed in Xenopus laevis oocytes.
Dresser, MJ; Gerstin, KM; Giacomini, KM; Gray, AT; Loo, DD, 2000
)
0.31
" PSAU has 100% oral bioavailability and is a powerful enhancer of the bioavailability of oral uridine."( Effect of 5-(phenylselenenyl)acyclouridine, an inhibitor of uridine phosphorylase, on plasma concentration of uridine released from 2',3',5'-tri-O-acetyluridine, a prodrug of uridine: relevance to uridine rescue in chemotherapy.
Ashour, OM; el Kouni, MH; Goudgaon, NM; Naguib, FN; Schinazi, RF, 2000
)
0.8
"The purpose of this investigation was to evaluate the effectiveness of oral 5-(phenylthio)acyclouridine (PTAU) in improving the oral bioavailability of uridine."( Enhancement of the bioavailability of oral uridine by coadministration of 5-(phenylthio)acyclouridine, a uridine phosphorylase inhibitor: implications for uridine rescue regimens in chemotherapy.
Al Safarjalani, ON; el Kouni, MH; Naguib, FN; Schinazi, RF; Shi, J; Zhou, XJ, 2001
)
0.79
" Coadministration of PTAU at 30, 45 and 60 mg/kg improved the low oral bioavailability (7."( Enhancement of the bioavailability of oral uridine by coadministration of 5-(phenylthio)acyclouridine, a uridine phosphorylase inhibitor: implications for uridine rescue regimens in chemotherapy.
Al Safarjalani, ON; el Kouni, MH; Naguib, FN; Schinazi, RF; Shi, J; Zhou, XJ, 2001
)
0.57
"The effectiveness of PTAU in improving the oral bioavailability of uridine could be useful in the rescue or protection from host toxicities of various chemotherapeutic pyrimidine analogues as well as in the management of medical disorders that are remedied by administration of uridine."( Enhancement of the bioavailability of oral uridine by coadministration of 5-(phenylthio)acyclouridine, a uridine phosphorylase inhibitor: implications for uridine rescue regimens in chemotherapy.
Al Safarjalani, ON; el Kouni, MH; Naguib, FN; Schinazi, RF; Shi, J; Zhou, XJ, 2001
)
0.81
"The purpose of this investigation was to evaluate the effectiveness of oral 5-(phenylthio)acyclouridine (PTAU) in improving the pharmacokinetics and bioavailability of oral uridine."( 5-(Phenylthio)acyclouridine: a powerful enhancer of oral uridine bioavailability: relevance to chemotherapy with 5-fluorouracil and other uridine rescue regimens.
Al Safarjalani, ON; El Kouni, MH; Naguib, FN; Rais, RH; Schinazi, RF; Shi, J; Zhou, XJ, 2005
)
0.87
" Coadministration of PTAU at 30, 45, 60, 120 and 240 mg/kg improved the low oral bioavailability (7."( 5-(Phenylthio)acyclouridine: a powerful enhancer of oral uridine bioavailability: relevance to chemotherapy with 5-fluorouracil and other uridine rescue regimens.
Al Safarjalani, ON; El Kouni, MH; Naguib, FN; Rais, RH; Schinazi, RF; Shi, J; Zhou, XJ, 2005
)
0.65
"The excellent pharmacokinetic properties of PTAU, and its extraordinary effectiveness in improving the oral bioavailability of uridine, could be useful to rescue or protect from host toxicities of 5-fluorouracil and various chemotherapeutic pyrimidine analogues used in the treatment of cancer and AIDS, as well as in the management of medical disorders that are remedied by the administration of uridine including CNS disorders (e."( 5-(Phenylthio)acyclouridine: a powerful enhancer of oral uridine bioavailability: relevance to chemotherapy with 5-fluorouracil and other uridine rescue regimens.
Al Safarjalani, ON; El Kouni, MH; Naguib, FN; Rais, RH; Schinazi, RF; Shi, J; Zhou, XJ, 2005
)
0.86
" The modulation of transporters during differentiation could potentially regulate drug bioavailability and cytotoxicity and should be evaluated prior to combining differentiating agents with traditional nucleoside analogs in the treatment of APL."( Nucleoside transporter expression and activity is regulated during granulocytic differentiation of NB4 cells in response to all-trans-retinoic acid.
Flanagan, SA; Meckling, KA, 2007
)
0.34
"34 g/kg/d), a dietary supplement with high bioavailability of uridine."( Uridine supplementation antagonizes zalcitabine-induced microvesicular steatohepatitis in mice.
Kirschner, J; Lebrecht, D; Setzer, B; Vargas-Infante, YA; Walker, UA, 2007
)
2.02
"Sixteen patients with lipoatrophy on stavudine-containing antiretroviral therapy were enrolled, and received NucleomaxX, a dietary supplement with a high bioavailability of uridine (36 g TID every other day for 16 weeks)."( Uridine supplementation in HIV lipoatrophy: pilot trial on safety and effect on mitochondrial indices.
Baron, E; Lebrecht, D; McComsey, GA; O'Riordan, M; Setzer, B; Walker, UA, 2008
)
1.98
" Hence, modulation of a specific nucleoside transporter may affect bioavailability and contribute significantly to sensitizing tumor cells to these anticancer agents."( Adenoviral-mediated overexpression of human equilibrative nucleoside transporter 1 (hENT1) enhances gemcitabine response in human pancreatic cancer.
Carbó, N; Casado, FJ; García-Manteiga, J; Mazo, A; Mercadé, E; Pastor-Anglada, M; Pérez-Torras, S, 2008
)
0.35
"NucleomaxX®, containing predominantly TAU, has significantly greater bioavailability than pure uridine in human subjects and may be useful in the management of mitochondrial toxicity."( Enhanced uridine bioavailability following administration of a triacetyluridine-rich nutritional supplement.
Cheung, P; Jacob, P; Mulligan, K; Roman, MC; Schambelan, M; Walker, UA; Weinberg, ME; Wen, M, 2011
)
1
"Gender differences have a significant impact on absorption, disposition and overall systemic bioavailability of various xenobiotics in rodents as well as humans."( Gender-dependent differences in uridine 5'-diphospho-glucuronosyltransferase have implications in metabolism and clearance of xenobiotics.
Hu, M; Kulkarni, K; Liu, W, 2013
)
0.67
" Furthermore, the article highlights the implications of sex hormone differences on metabolic clearance and thereby oral bioavailability of xenobiotics that are predominantly metabolized by UGTs in vivo."( Gender-dependent differences in uridine 5'-diphospho-glucuronosyltransferase have implications in metabolism and clearance of xenobiotics.
Hu, M; Kulkarni, K; Liu, W, 2013
)
0.67
" These differences significantly affect the metabolic clearance and the systemic bioavailability of compounds eliminated via this disposition pathway."( Gender-dependent differences in uridine 5'-diphospho-glucuronosyltransferase have implications in metabolism and clearance of xenobiotics.
Hu, M; Kulkarni, K; Liu, W, 2013
)
0.67
"Decitabine, a DNA methyltransferase 1 inhibitor or DNA hypomethylating compound, is not readily orally bioavailable because of rapid clearance by cytidine deaminase (CDA) in the gut and liver."( An oral fixed-dose combination of decitabine and cedazuridine in myelodysplastic syndromes: a multicentre, open-label, dose-escalation, phase 1 study.
Amrein, PC; Azab, M; DeZern, AE; Faderl, S; Garcia-Manero, G; Harb, W; Kantarjian, H; Lowder, J; Michaelis, LC; Odenike, O; Oganesian, A; Savona, MR; Steensma, DP, 2019
)
0.76
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
"Capecitabine is an orally bioavailable prodrug of the chemotherapeutic agent, fluorouracil."( Real-time comprehensive toxicology testing in the clinical management of accidental pediatric capecitabine ingestion.
Badea, A; Garcia, E; Gintjee, TJ; Goodnough, R; Li, K; Lynch, KL; Repplinger, D, 2020
)
0.56
"To determine if an oral dosing strategy might be feasible in the clinic with AZA, we attempted to increase the bioavailability of oral AZA through the use of CDZ, in a murine model."( Oral Azacitidine and Cedazuridine Approximate Parenteral Azacitidine Efficacy in Murine Model.
Arrate, M; Azab, M; Boyd, K; Fuller, L; Gorska, AE; Keer, H; Oganesian, A; Ramsey, HE; Savona, MR, 2020
)
0.86
" The development of oral HMAs has been an area of active interest; however, oral bioavailability has been quite poor due to rapid metabolism by cytidine deaminase (CDA)."( Cedazuridine/decitabine: from preclinical to clinical development in myeloid malignancies.
Cahill, K; Odenike, O; Patel, AA; Saygin, C, 2021
)
1.14

Dosage Studied

The increase in [3H]uridine transport was nuclear receptor-mediated. Dose-response curves studies suggested that inosine, but not uridine, has a common receptor site with epinephrine in adipose tissue.

ExcerptRelevanceReference
" No cortisol-resistant cells could be distinguished, and dose-response curves for a number of glucocorticoids showed a correlation to the saturation of the glucocorticoid receptors."( Dissociation between cortisol-induced pycnosis and inhibition of [3H]uridine incorporation in rat thymocytes.
Engelhardt, M, 1977
)
0.49
" Dose-response curves studies suggested that inosine, but not uridine, has a common receptor site with epinephrine in adipose tissue."( Effects of uridine and inosine on glucose metabolism in skeletal muscle and activated lipolysis in adipose tissue.
Hait, G; Kypson, J, 1976
)
0.89
" The dosage blood loss (25 ml of blood) would prevent the inhibition of lymphocytic blasttransformation reaction, that seems to prove the functional nature of metabolic immunosuppression, induced by the increased concentration of fatty acids in blood due to hydrolysis of administered triglycerides."( [Supression of the lymphocyte blast transformation reaction evoked in human subjects by a fat load].
Dil'man, VM; Fedorov, SN; Poroshina, TE; Vishnevskiĭ, AS, 1979
)
0.26
" The equivalence of CHO and CdR in dose-response in terms of stimulated RNA synthesis and their disparity in dose-response in terms of cytotoxic effects indicate that the systems involved in conferring protection against the lethal effects of Cd2+ are not similarly involved in attenuating the effects on RNA metabolism."( Cadmium-induced alterations in RNA metabolism in cultures of Chinese hamster cells sensitive to and resistant to the cytotoxic effects of cadmium.
Campbell, EW; Enger, MD; Hildebrand, CE; Kissane, RJ; Ratliff, RL; Tobey, RA, 1979
)
0.26
" The replicative and transcriptive activities of the two arms have been examined in order to understand how such phylogenetically different components of the X contribute toward the chromosomal basis of dosage compensation."( Hyperactivity and faster replicating property of the two arms of the male X of Drosophila pseudoobscura.
Chatterjee, SN; Mukherjee, AS, 1976
)
0.26
" This gene dosage independence of the synthesis rate of r-protein was similar to that observed earlier for the synthesis of ribosomal ribonucleic acid (rRNA)."( Regulation of ribosomal protein synthesis in Escherichia coli B/r.
Dennis, PP; Young, RF, 1975
)
0.25
" If two distinct populations are necessary to the full expression of phiX memory, both populations recirculate because the memory cells in lymph draining the sites of the primary response and those reaching the central lymph of adoptive hosts give parallel dose-response curves."( The properities of lymphocytes which carry immunologic memory of phiX 174.
Mackaness, GB; McGregor, DD, 1975
)
0.25
" Injection of protein or glycoprotein precursors into one Rc produced heavy labeling of both Rcs including their processes; a slight labeling of other ganglion compartments was only found after increasing the dosage of the amino acids glycine and leucine."( Transfer of radioactive material between electrically coupled neurons of the leech central nervous system.
Kreutzberg, GW; Rieske, E; Schubert, P, 1975
)
0.25
" Mercury ion-induced antifertility effects at the dosage used in these experiments are reversible."( Effects of mercury on spermatogenesis studied by velocity sedimentation cell separation and serial mating.
Dixon, RL; Lee, IP, 1975
)
0.25
" No teratogenic effects were visible with the dosage schedules used."( Effects of delta9-tetrahydrocannabinol and ethanol on body weight protein and nucleic acid synthesis in chick embryos.
Jakubović, A; McGeer, PL, 1976
)
0.26
" Probit plots of the dose-response data obtained for each resistant 2008 line following chronic exposure to PALA again confirmed this prediction."( Mechanism-based model for tumor drug resistance.
Chan, TC; Kuczek, T, 1992
)
0.28
"The present study was carried out to investigate the time course of metabolization in brain and the influence on RNA synthesis of a retention-improving dosage of methylglucamine orotate after intracerebroventricular application."( Metabolization of a retention-improving dosage of methylglucamine orotate in rat brain.
Matthies, H; Popov, N; Staak, S; Tischmeyer, W, 1990
)
0.28
" Dose-response curves for each agent indicate the following absolute potency: FUDR greater than FUR greater than ARA-C greater than 5-FU = bleomycin greater than DFUR."( Evaluation of antiproliferative agents using a cell-culture model.
Senderoff, RI; Smith, DR; Sokoloski, TD; Weber, PA, 1990
)
0.28
"Maximal dosing of cytotoxic chemotherapy drugs is often limited by the development of severe nonmyelosuppressive toxicities."( Chemoprotectants for cancer chemotherapy.
Dorr, RT, 1991
)
0.28
" That this increase in [3H]uridine transport was nuclear receptor-mediated is supported by the excellent correspondence of the L-T3 dose-response curve for [3H]uridine uptake and that for L-T3 binding to receptor."( Stimulation of facilitated [3H]uridine transport by thyroid hormone in GH1 cells. Evidence for regulation by the thyroid hormone nuclear receptor.
Samuels, HH; Stanley, F; Tsai, JS, 1986
)
0.85
" The results are discussed in the light of behavioural findings in which intraperitoneally applied D-galactosamine at this dosage improves the retention performance of an acquired behaviour in the rat."( Effects of intraperitoneally applied D-galactosamine on uridine and cytidine plasma content and brain activity of uridine kinase in the rat.
Matthies, H; Popov, N; Staak, S, 1989
)
0.52
" In tumor tissue, optimal doses of FUra or FdUrd resulted in lower (a) FdUMP levels (5- to 2-fold), (b) RNA-level antimetabolites (6- to 3-fold), and (c) DNA-level antimetabolites (10- to 4-fold) compared to an optimal dosage of FdCyd plus H4Urd."( Tumor-selective metabolism of 5-fluoro-2'-deoxycytidine coadministered with tetrahydrouridine compared to 5-fluorouracil in mice bearing Lewis lung carcinoma.
Boothman, DA; Briggle, TV; Greer, S, 1987
)
0.5
" The dose-response curve for the inhibition of uridine transport by nitrobenzylthioinosine (NBMPR) was biphasic: approx."( Nucleoside transport in rat cerebral-cortical synaptosomes. Evidence for two types of nucleoside transporters.
Jarvis, SM; Lee, CW, 1988
)
0.53
"The dose-response effects of intracerebroventricular (ICV) infusion of the pyrimidine ribonucleosides cytidine and uridine and the purine ribonucleoside adenosine on sleep and wakefulness (W) in rats were examined and compared."( A comparison of the dose response effects of pyrimidine ribonucleosides and adenosine on sleep in rats.
Crane, RA; Radulovacki, M; Rapoza, D; Virus, RM, 1985
)
0.48
" The dose-response curves of these chemicals were similar to those of other known tumor promoters on Chinese hamster V79 cells."( Inhibition of gap junctional intercellular communication in human teratocarcinoma cells by organochlorine pesticides.
Chang, CC; Kavanagh, T; Lin, ZX; Trosko, JE, 1986
)
0.27
" A linear dose-response regression curve was obtained by plotting the log of the amount of RNA made, expressed as a percentage of the control, versus the log of the reciprocal of the interferon dilution."( Rapid sensitive assay for interferons based on the inhibition of MM virus nucleic acid synthesis.
Allen, PT; Giron, DJ, 1970
)
0.25
" Different dose-response curves were obtained for cytostasis and inhibition of [(3)H]-nucleoside incorporation, and changes in [(3)H]thymidine uptake were detected within 15 min of treatment with the inhibitors."( Rapid changes in nucleoside transport induced by growth inhibitors. Studies with neoplastic mast cells.
Lingwood, CA; Thomas, DB, 1974
)
0.25
" A time-response and a dose-response study showed that actinomycin D inhibits pulmonary RNA synthesis as efficiently as hepatic RNA synthesis."( Qualitative and quantitative aspects of the biosynthesis of ribonucleic acid and of protein in the liver and the lung of the Syrian golden hamster.
Witschi, H, 1973
)
0.25
" However, actinomycin D, at a dosage of 250 mug/mouse in vivo and 10 mug/ml in vitro produces breakdown of labeled RNA, thus confirming earlier observations that the drug is not a suitable tool for RNA kinetics determinations."( Pulse labeling of RNA of mammalian cells.
Baserga, R; Berman, S; Rovera, G, 1970
)
0.25
" In dose-response studies, increases in cell membrane permeability, measured as the loss of K+ ions, occurred along with the stimulation of [3H]uridine incorporation into RNA."( Stimulatory, permeabilizing, and toxic effects of amphotericin B on L cells.
Brajtburg, J; Elberg, S; Kobayashi, GS; Medoff, G; Medoff, J; Schlessinger, D, 1984
)
0.47
" The dose-response curve was steep, nearly all incorporation being inhibited by 2 x IC50."( Inhibition of lymphocyte transformation by mepacrine and chloroquine.
Trist, DG; Weatherall, M, 1981
)
0.26
" In a comparative study with this 3-day dosage schedule, the efficacy of daily doses of 50 mg of FMAU per kg was greater than that of the same doses of FIAC and FIAU, in that order; all these were more effective than daily doses of 50, 100, or 200 mg of acyclovir or of 500 mg of phosphonoformic acid per kg."( Treatment of primary acute genital herpes in guinea pigs by intraperitoneal administration of fluoropyrimidines.
Hsiung, GD; Mayo, DR, 1984
)
0.27
" Drosophila melanogaster has a comparable system of dosage compensation."( Insect sex chromosomes. VI. A presumptive hyperactivation of the male X chromosome in Acheta domesticus (L.).
Ali, S; Rao, SR, 1982
)
0.26
" Low dose and either continuous infusion or repetitive dosing of leucovorin, as well as the effect of treatment sequence and intervals between drugs, require additional investigation."( Preclinical and clinical aspects of biomodulation of 5-fluorouracil.
Allegra, CJ; Grogan, L; Sotos, GA, 1994
)
0.29
" Dose-response curve for the inhibition of equilibrative uridine transport by N-ethylmaleimide (NEM), a sulfhydryl reagent, in these cells was biphasic."( Sensitivity to inhibition by N-ethylmaleimide: a property of nitrobenzylthioinosine-sensitive equilibrative nucleoside transporter of murine myeloma cells.
Goh, LB; Lee, CW; Tu, Y, 1995
)
0.54
" Dose-response characteristics of the inhibition were determined."( Cyclopentenyl uracil: an effective inhibitor of uridine salvage in vivo.
August, EM; Cysyk, RL; Malinowski, N; Marquez, V; Moyer, JD; Zaharevitz, D, 1995
)
0.55
"The dose-response curves for the inhibition of equilibrative uridine transport by dilazep, dipyridamole and nitrobenzylthioinosine (NBMPR) in undifferentiated HL-60 cells were biphasic."( Decrease in equilibrative uridine transport during monocytic differentiation of HL-60 leukaemia: involvement of protein kinase C.
Lee, CW, 1994
)
0.83
" The recommended 5-FU dosage for phase II evaluations is 1,250 mg/m(2)/wk for 3 weeks every 4 weeks with the intensified PN401 dose schedule (schedule 2)."( Phase I and pharmacologic study of PN401 and fluorouracil in patients with advanced solid malignancies.
Campbell, E; Davidson, K; Diab, SG; Drengler, RL; Eckhardt, SG; Garner, AM; Hammond, LA; Hidalgo, M; Louie, A; O'Neil, JD; Rodriguez, G; Rowinsky, EK; Villalona-Calero, MA; von Borstel, R; Von Hoff, DD; Weiss, G, 2000
)
0.31
" Dose-response studies in fibroblasts indicated that the majority of the suppressive effect required concentrations characteristic of cell-surface GC receptors, a point confirmed by persistent DEX-induced suppression in the presence of RU486, an antagonist of classic cytosolic steroid hormone receptors."( Glucocorticoids induce a near-total suppression of hyaluronan synthase mRNA in dermal fibroblasts and in osteoblasts: a molecular mechanism contributing to organ atrophy.
Liu, C; Watson, CE; Werth, VP; Williams, KJ; Zhang, W, 2000
)
0.31
" Forced expiratory volume in 1 sec (FEV(1)) profiles following dosing were similar across treatment groups, with some acute, reversible decline seen in both groups, most notably in subjects with lower lung function at baseline."( Safety and tolerability of denufosol tetrasodium inhalation solution, a novel P2Y2 receptor agonist: results of a phase 1/phase 2 multicenter study in mild to moderate cystic fibrosis.
Daines, C; Deterding, R; Engels, J; Gibson, R; Gorden, J; Lavange, L; Marshall, B; Mathews, D; Milgram, L; Milla, C; Ramsey, B; Retsch-Bogart, G; Schaberg, A; Williams, J; Zeitlin, PL, 2005
)
0.33
" All three slowed the rate of RNA decay in a dose-response fashion, they were specific to the b-ARE, and two of them were individually effective."( Increased Bcl2 expression by antisense oligoribonucleotides targeting the adenine-uridine-rich element motif.
Bevilacqua, A; Canti, G; Capaccioli, S; Ghisolfi, L; Lapucci, A; Nicolin, A; Papucci, L; Schiavone, N; Tataranni, G, 2005
)
0.55
"36 mg/kg/d of zalcitabine (corresponding to human dosing adapted for body surface), or 13 mg/kg/d of zalcitabine."( Uridine supplementation antagonizes zalcitabine-induced microvesicular steatohepatitis in mice.
Kirschner, J; Lebrecht, D; Setzer, B; Vargas-Infante, YA; Walker, UA, 2007
)
1.78
" All treatments were generally well tolerated, with no dose-response trends observed with respect to safety parameters."( Phase 2 randomized safety and efficacy trial of nebulized denufosol tetrasodium in cystic fibrosis.
Brody, AS; Coquillette, SJ; Deterding, RR; Engels, JM; Lavange, LM; Mathews, DW; Millard, SP; Ramsey, BW, 2007
)
0.34
" Downregulation of a GAL1-TRM112 allele protects against zymocin whereas LYS9, TRM11 and MTQ2 are dosage suppressors of zymocin."( tRNA and protein methylase complexes mediate zymocin toxicity in yeast.
Bär, C; Jablonowski, D; Schaffrath, R; Studte, P; Tuite, MF; von der Haar, T; Zink, S, 2008
)
0.35
" UTP at doses between 500 and 3000 microM resulted in increasing cell death following a normal sigmoid dose-response model."( Cell death induced by uridine 5'-triphosphate (UTP) in contrast to adenosine 5'-triphosphate (ATP) in human epidermoid carcinoma cells (A-431).
Neuhuber, W; Ogilvie, A; Völkl, T, 2008
)
0.66
" Single and repeated dosing with NucleomaxX® resulted in peak plasma uridine concentrations 1-2 hours later of 150."( Enhanced uridine bioavailability following administration of a triacetyluridine-rich nutritional supplement.
Cheung, P; Jacob, P; Mulligan, K; Roman, MC; Schambelan, M; Walker, UA; Weinberg, ME; Wen, M, 2011
)
1.02
" Atenolol inhibited the increase in HR at a small dosage of higenamine but potentiated it at a higher dosage."( Hypotensive and cardio-chronotropic constituents of Tinospora crispa and mechanisms of action on the cardiovascular system in anesthetized rats.
Andersen, RJ; Jansakul, C; Mulvany, MJ; Praman, S; Williams, DE, 2012
)
0.38
" To further delineate the mechanism of action for Vido, rats were dosed concomitantly with uridine (Uri)."( Vidofludimus inhibits colonic interleukin-17 and improves hapten-induced colitis in rats by a unique dual mode of action.
Ammendola, A; Doblhofer, R; Fitzpatrick, LR; Small, JS, 2012
)
0.6
" We detected 83 synthetic dosage interactions with actin, 78 resulted in reduced growth, whereas in 5 cases overexpression of actin suppressed the growth defects caused by the deleted genes."( Actin dosage lethality screening in yeast mediated by selective ploidy ablation reveals links to urmylation/wobble codon recognition and chromosome stability.
Amberg, D; Burke, D; Cho, J; Cortese, M; Haarer, B; Mi-Mi, L; Viggiano, S, 2013
)
0.39
" At a daily dosage of 400 mg/kg, fenofibrate treatment causes reduction of liver NAD(+)/NADH ratio, induces hyper-acetylation of peroxisomal bifunctional enzyme (ECHD) and acyl-CoA oxidase 1 (ACOX1), and induces excessive accumulation of long chain fatty acids (LCFA) and very long chain fatty acids (VLCFA)."( Uridine prevents fenofibrate-induced fatty liver.
Le, TT; Pizzorno, G; Urasaki, Y, 2014
)
1.85
" Life-threatening 5-FU overdoses occur because of infusion pump errors, dosage miscalculations, and accidental or suicidal ingestion of capecitabine."( Emergency use of uridine triacetate for the prevention and treatment of life-threatening 5-fluorouracil and capecitabine toxicity.
Bamat, MK; Cartwright, TH; El-Rayes, BF; Fakih, MG; King, TR; Ma, WW; Posey, JA; Saif, MW; von Borstel, RW, 2017
)
0.79
" These findings show that, when assessing plasma uracil and dihydrouracil levels for adaptive fluoropyrimidine dosing in clinical practice, sampling should be done between 8:00 h and 9:00 h after overnight fasting to avoid bias caused by circadian rhythm and food effects."( Food-effect study on uracil and dihydrouracil plasma levels as marker for dihydropyrimidine dehydrogenase activity in human volunteers.
Beijnen, JH; Cats, A; de Vries, N; Guchelaar, HJ; Henricks, LM; Huitema, ADR; Jacobs, BAW; Meulendijks, D; Pluim, D; Rosing, H; Schellens, JHM; van den Broek, D, 2018
)
0.48
"The purpose of this study was to investigate the safety, tolerability, and pharmacokinetic profile of sofosbuvir and its metabolites after a single dose of sofosbuvir 400mg and once daily dosing of sofosbuvir 400mg for 7days in healthy Chinese subjects."( Pharmacokinetics, Safety, and Tolerability of the Direct-acting Hepatitis C Antiviral Sofosbuvir in HealthyChineseSubjects.
Brainard, DM; Chen, G; Chen, H; Ding, Y; Li, X; Massetto, B; Niu, J; Shen, G; Zhang, H; Zhu, X, 2018
)
0.48
" Steady state of the major metabolite GS-331007 was achieved after 4days of consecutive dosing with sofosbuvir 400mg once daily."( Pharmacokinetics, Safety, and Tolerability of the Direct-acting Hepatitis C Antiviral Sofosbuvir in HealthyChineseSubjects.
Brainard, DM; Chen, G; Chen, H; Ding, Y; Li, X; Massetto, B; Niu, J; Shen, G; Zhang, H; Zhu, X, 2018
)
0.48
" The PK parameters of sofosbuvir and its metabolite (GS-331007) in both blood and urine samples were analyzed after dosing by the established liquid chromatography tandem mass spectrometry analytical method."( Pharmacokinetic Profile of a Generic Formulation of Sofosbuvir and Its Metabolite GS-331007 in Healthy Chinese Subjects.
Chen, G; Chen, H; Ding, Y; Li, X; Niu, J; Shen, Z; Zhang, H; Zhu, X, 2019
)
0.51
"To determine if an oral dosing strategy might be feasible in the clinic with AZA, we attempted to increase the bioavailability of oral AZA through the use of CDZ, in a murine model."( Oral Azacitidine and Cedazuridine Approximate Parenteral Azacitidine Efficacy in Murine Model.
Arrate, M; Azab, M; Boyd, K; Fuller, L; Gorska, AE; Keer, H; Oganesian, A; Ramsey, HE; Savona, MR, 2020
)
0.86
"Following pharmacokinetic and pharmacodynamic assessment of oral AZA dosed with CDZ in murine and monkey models, we tested this regimen in vivo with a human cell line-derived xenograft transplantation experiment (CDX)."( Oral Azacitidine and Cedazuridine Approximate Parenteral Azacitidine Efficacy in Murine Model.
Arrate, M; Azab, M; Boyd, K; Fuller, L; Gorska, AE; Keer, H; Oganesian, A; Ramsey, HE; Savona, MR, 2020
)
0.86
"FOLFIRINOX and FOLFOXIRI are combination chemotherapy treatments that incorporate the same drug cocktail (folinic acid, 5-fluorouracil, oxaliplatin and irinotecan) but exploit an altered dosing regimen when used in the management of pancreatic and colorectal cancer, respectively."( A single microbubble formulation carrying 5-fluorouridine, Irinotecan and oxaliplatin to enable FOLFIRINOX treatment of pancreatic and colon cancer using ultrasound targeted microbubble destruction.
Callan, B; Callan, JF; Gao, J; Griffith, DM; Logan, KA; Love, M; McHale, AP; McKaig, T; Nesbitt, H; Taylor, M, 2021
)
0.87
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
fundamental metaboliteAny metabolite produced by all living cells.
drug metabolitenull
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
uridines
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (31)

PathwayProteinsCompounds
Pyrimidine Metabolism2353
beta-Ureidopropionase Deficiency2353
UMP Synthase Deficiency (Orotic Aciduria)2353
Dihydropyrimidinase Deficiency2353
MNGIE (Mitochondrial Neurogastrointestinal Encephalopathy)2353
Pyrimidine Ribonucleosides Degradation511
UTP and CTP dephosphorylation I113
pyrimidine ribonucleosides salvage I29
superpathway of pyrimidine ribonucleosides salvage720
pyrimidine ribonucleosides salvage II27
pyrimidine salvage pathway311
Pyrimidine Nucleotides and Nucleosides metabolism ( Pyrimidine Nucleotides and Nucleosides metabolism )4549
Uridine + Orthophosphate = Uracil + D-Ribose 1-phosphate ( Pyrimidine Nucleotides and Nucleosides metabolism )13
Biomarkers for pyrimidine metabolism disorders1432
Urea cycle and associated pathways2430
Renz2020 - GEM of Human alveolar macrophage with SARS-CoV-20490
Pyrimidine synthesis and deprivation pathway (COVID-19 Disease Maps)1329
15q25 copy number variation08
pyrimidine ribonucleosides degradation513
nucleoside and nucleotide degradation (archaea)722
superpathway of pyrimidine deoxyribonucleoside salvage2222
superpathway of pyrimidine ribonucleosides salvage2237
pyrimidine ribonucleosides salvage I613
pyrimidine ribonucleosides salvage II812
pyrimidine deoxyribonucleosides salvage1517
superpathway of pyrimidine ribonucleosides degradation1317
UTP and CTP dephosphorylation I314
salvage pathways of pyrimidine ribonucleotides936
pyrimidine ribonucleosides degradation II28
pyrimidine salvage pathway611
superpathway of ribose and deoxyribose phosphate degradation024
(deoxy)ribose phosphate degradation018
purine and pyrimidine metabolism032
salvage pathways of purine and pyrimidine nucleotides030
pyrimidine ribonucleosides degradation I07
Biochemical pathways: part I0466
Pyrimidine metabolism038
Pyrimidine metabolism and related diseases1844

Protein Targets (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency50.11870.003245.467312,589.2998AID2517
phosphopantetheinyl transferaseBacillus subtilisPotency96.37500.141337.9142100.0000AID1490
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency12.58930.28189.721235.4813AID2326
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
gemininHomo sapiens (human)Potency1.25890.004611.374133.4983AID624297
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency125.89206.309660.2008112.2020AID720707
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Cytidine DeaminaseEscherichia coliKi800.0000800.0000800.0000800.0000AID977610
Sodium/nucleoside cotransporter 1Homo sapiens (human)IC50 (µMol)5.80005.50005.65005.8000AID1222907
Sodium/nucleoside cotransporter 1Homo sapiens (human)Ki5.20001.80003.50005.2000AID1222907
Sodium/nucleoside cotransporter 2Homo sapiens (human)IC50 (µMol)32.00005.50005.50005.5000AID1222908
Sodium/nucleoside cotransporter 2Homo sapiens (human)Ki31.00005.30005.30005.3000AID1222908
Cytidine deaminaseHomo sapiens (human)Ki0.00000.00001.43332.3000AID55389
Protein cereblonHomo sapiens (human)IC50 (µMol)757.00000.28601.70663.0000AID1685005
Protein cereblonHomo sapiens (human)Ki390.00001.49006.580010.0000AID1685005
Equilibrative nucleoside transporter 1Homo sapiens (human)IC50 (µMol)52.00000.00013.688363.0000AID1222905
Equilibrative nucleoside transporter 1Homo sapiens (human)Ki51.00000.00040.10381.1000AID1222905
Solute carrier family 28 member 3Homo sapiens (human)IC50 (µMol)5.40003.30004.35005.4000AID1222909
Solute carrier family 28 member 3Homo sapiens (human)Ki3.40002.10002.75003.4000AID1222909
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (71)

Processvia Protein(s)Taxonomy
cytidine transportSodium/nucleoside cotransporter 1Homo sapiens (human)
uridine transmembrane transportSodium/nucleoside cotransporter 1Homo sapiens (human)
azole transmembrane transportSodium/nucleoside cotransporter 1Homo sapiens (human)
pyrimidine-containing compound transmembrane transportSodium/nucleoside cotransporter 1Homo sapiens (human)
nucleoside import across plasma membraneSodium/nucleoside cotransporter 1Homo sapiens (human)
nucleoside transmembrane transportSodium/nucleoside cotransporter 1Homo sapiens (human)
purine nucleobase transmembrane transportSodium/nucleoside cotransporter 1Homo sapiens (human)
pyrimidine nucleobase transportSodium/nucleoside cotransporter 1Homo sapiens (human)
nucleobase-containing compound metabolic processSodium/nucleoside cotransporter 2Homo sapiens (human)
xenobiotic metabolic processSodium/nucleoside cotransporter 2Homo sapiens (human)
neurotransmitter transportSodium/nucleoside cotransporter 2Homo sapiens (human)
xenobiotic transmembrane transportSodium/nucleoside cotransporter 2Homo sapiens (human)
pyrimidine nucleobase transportSodium/nucleoside cotransporter 2Homo sapiens (human)
purine nucleoside transmembrane transportSodium/nucleoside cotransporter 2Homo sapiens (human)
uridine transmembrane transportSodium/nucleoside cotransporter 2Homo sapiens (human)
adenosine transportSodium/nucleoside cotransporter 2Homo sapiens (human)
inosine transportSodium/nucleoside cotransporter 2Homo sapiens (human)
azole transmembrane transportSodium/nucleoside cotransporter 2Homo sapiens (human)
pyrimidine-containing compound transmembrane transportSodium/nucleoside cotransporter 2Homo sapiens (human)
transport across blood-brain barrierSodium/nucleoside cotransporter 2Homo sapiens (human)
nucleoside transmembrane transportSodium/nucleoside cotransporter 2Homo sapiens (human)
purine nucleobase transmembrane transportSodium/nucleoside cotransporter 2Homo sapiens (human)
retina homeostasisSodium/nucleoside cotransporter 2Homo sapiens (human)
angiogenesisRap guanine nucleotide exchange factor 3Homo sapiens (human)
adaptive immune responseRap guanine nucleotide exchange factor 3Homo sapiens (human)
signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 3Homo sapiens (human)
associative learningRap guanine nucleotide exchange factor 3Homo sapiens (human)
Rap protein signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of actin cytoskeleton organizationRap guanine nucleotide exchange factor 3Homo sapiens (human)
negative regulation of syncytium formation by plasma membrane fusionRap guanine nucleotide exchange factor 3Homo sapiens (human)
intracellular signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of GTPase activityRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of angiogenesisRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of angiogenesisRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of protein export from nucleusRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of stress fiber assemblyRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of syncytium formation by plasma membrane fusionRap guanine nucleotide exchange factor 3Homo sapiens (human)
establishment of endothelial barrierRap guanine nucleotide exchange factor 3Homo sapiens (human)
cellular response to cAMPRap guanine nucleotide exchange factor 3Homo sapiens (human)
Ras protein signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of insulin secretionRap guanine nucleotide exchange factor 3Homo sapiens (human)
cell surface receptor signaling pathwayCytidine deaminaseHomo sapiens (human)
pyrimidine-containing compound salvageCytidine deaminaseHomo sapiens (human)
cytidine deaminationCytidine deaminaseHomo sapiens (human)
cytosine metabolic processCytidine deaminaseHomo sapiens (human)
negative regulation of cell growthCytidine deaminaseHomo sapiens (human)
UMP salvageCytidine deaminaseHomo sapiens (human)
negative regulation of nucleotide metabolic processCytidine deaminaseHomo sapiens (human)
response to cycloheximideCytidine deaminaseHomo sapiens (human)
cellular response to external biotic stimulusCytidine deaminaseHomo sapiens (human)
neurotransmitter uptakeEquilibrative nucleoside transporter 2Homo sapiens (human)
neurotransmitter transportEquilibrative nucleoside transporter 2Homo sapiens (human)
xenobiotic transmembrane transportEquilibrative nucleoside transporter 2Homo sapiens (human)
nucleobase transportEquilibrative nucleoside transporter 2Homo sapiens (human)
adenine transportEquilibrative nucleoside transporter 2Homo sapiens (human)
nucleoside transportEquilibrative nucleoside transporter 2Homo sapiens (human)
purine nucleoside transmembrane transportEquilibrative nucleoside transporter 2Homo sapiens (human)
cytidine transportEquilibrative nucleoside transporter 2Homo sapiens (human)
uridine transmembrane transportEquilibrative nucleoside transporter 2Homo sapiens (human)
adenosine transportEquilibrative nucleoside transporter 2Homo sapiens (human)
inosine transportEquilibrative nucleoside transporter 2Homo sapiens (human)
hypoxanthine transportEquilibrative nucleoside transporter 2Homo sapiens (human)
thymine transportEquilibrative nucleoside transporter 2Homo sapiens (human)
pyrimidine-containing compound transmembrane transportEquilibrative nucleoside transporter 2Homo sapiens (human)
transport across blood-brain barrierEquilibrative nucleoside transporter 2Homo sapiens (human)
nucleoside transmembrane transportEquilibrative nucleoside transporter 2Homo sapiens (human)
guanine transmembrane transportEquilibrative nucleoside transporter 2Homo sapiens (human)
uracil transmembrane transportEquilibrative nucleoside transporter 2Homo sapiens (human)
purine nucleobase transmembrane transportEquilibrative nucleoside transporter 2Homo sapiens (human)
guanine transportEquilibrative nucleoside transporter 2Homo sapiens (human)
protein ubiquitinationProtein cereblonHomo sapiens (human)
positive regulation of Wnt signaling pathwayProtein cereblonHomo sapiens (human)
negative regulation of protein-containing complex assemblyProtein cereblonHomo sapiens (human)
positive regulation of protein-containing complex assemblyProtein cereblonHomo sapiens (human)
negative regulation of monoatomic ion transmembrane transportProtein cereblonHomo sapiens (human)
locomotory exploration behaviorProtein cereblonHomo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processProtein cereblonHomo sapiens (human)
neurotransmitter uptakeEquilibrative nucleoside transporter 1Homo sapiens (human)
nucleobase-containing compound metabolic processEquilibrative nucleoside transporter 1Homo sapiens (human)
xenobiotic metabolic processEquilibrative nucleoside transporter 1Homo sapiens (human)
neurotransmitter transportEquilibrative nucleoside transporter 1Homo sapiens (human)
xenobiotic transmembrane transportEquilibrative nucleoside transporter 1Homo sapiens (human)
lactationEquilibrative nucleoside transporter 1Homo sapiens (human)
nucleobase transportEquilibrative nucleoside transporter 1Homo sapiens (human)
adenine transportEquilibrative nucleoside transporter 1Homo sapiens (human)
nucleoside transportEquilibrative nucleoside transporter 1Homo sapiens (human)
purine nucleoside transmembrane transportEquilibrative nucleoside transporter 1Homo sapiens (human)
cytidine transportEquilibrative nucleoside transporter 1Homo sapiens (human)
uridine transmembrane transportEquilibrative nucleoside transporter 1Homo sapiens (human)
adenosine transportEquilibrative nucleoside transporter 1Homo sapiens (human)
inosine transportEquilibrative nucleoside transporter 1Homo sapiens (human)
hypoxanthine transportEquilibrative nucleoside transporter 1Homo sapiens (human)
thymine transportEquilibrative nucleoside transporter 1Homo sapiens (human)
excitatory postsynaptic potentialEquilibrative nucleoside transporter 1Homo sapiens (human)
cellular response to glucose stimulusEquilibrative nucleoside transporter 1Homo sapiens (human)
cellular response to hypoxiaEquilibrative nucleoside transporter 1Homo sapiens (human)
pyrimidine-containing compound transmembrane transportEquilibrative nucleoside transporter 1Homo sapiens (human)
transport across blood-brain barrierEquilibrative nucleoside transporter 1Homo sapiens (human)
nucleoside transmembrane transportEquilibrative nucleoside transporter 1Homo sapiens (human)
guanine transmembrane transportEquilibrative nucleoside transporter 1Homo sapiens (human)
uracil transmembrane transportEquilibrative nucleoside transporter 1Homo sapiens (human)
pyrimidine nucleobase transmembrane transportEquilibrative nucleoside transporter 1Homo sapiens (human)
purine nucleobase transmembrane transportEquilibrative nucleoside transporter 1Homo sapiens (human)
CMP biosynthetic processUridine-cytidine kinase 1 Homo sapiens (human)
UMP salvageUridine-cytidine kinase 1 Homo sapiens (human)
CTP salvageUridine-cytidine kinase 1 Homo sapiens (human)
xenobiotic metabolic processSolute carrier family 28 member 3Homo sapiens (human)
xenobiotic transmembrane transportSolute carrier family 28 member 3Homo sapiens (human)
pyrimidine nucleobase transportSolute carrier family 28 member 3Homo sapiens (human)
uridine transmembrane transportSolute carrier family 28 member 3Homo sapiens (human)
sodium ion transmembrane transportSolute carrier family 28 member 3Homo sapiens (human)
pyrimidine-containing compound transmembrane transportSolute carrier family 28 member 3Homo sapiens (human)
nucleoside transmembrane transportSolute carrier family 28 member 3Homo sapiens (human)
purine nucleobase transmembrane transportSolute carrier family 28 member 3Homo sapiens (human)
pyrimidine nucleoside transportSolute carrier family 28 member 3Homo sapiens (human)
purine nucleoside transmembrane transportSolute carrier family 28 member 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (28)

Processvia Protein(s)Taxonomy
purine nucleobase transmembrane transporter activitySodium/nucleoside cotransporter 1Homo sapiens (human)
nucleoside:sodium symporter activitySodium/nucleoside cotransporter 1Homo sapiens (human)
cytidine transmembrane transporter activitySodium/nucleoside cotransporter 1Homo sapiens (human)
uridine transmembrane transporter activitySodium/nucleoside cotransporter 1Homo sapiens (human)
pyrimidine- and adenosine-specific:sodium symporter activitySodium/nucleoside cotransporter 1Homo sapiens (human)
azole transmembrane transporter activitySodium/nucleoside cotransporter 1Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium/nucleoside cotransporter 2Homo sapiens (human)
purine nucleobase transmembrane transporter activitySodium/nucleoside cotransporter 2Homo sapiens (human)
nucleoside:sodium symporter activitySodium/nucleoside cotransporter 2Homo sapiens (human)
purine nucleoside transmembrane transporter activitySodium/nucleoside cotransporter 2Homo sapiens (human)
uridine transmembrane transporter activitySodium/nucleoside cotransporter 2Homo sapiens (human)
pyrimidine- and adenosine-specific:sodium symporter activitySodium/nucleoside cotransporter 2Homo sapiens (human)
azole transmembrane transporter activitySodium/nucleoside cotransporter 2Homo sapiens (human)
guanyl-nucleotide exchange factor activityRap guanine nucleotide exchange factor 3Homo sapiens (human)
protein bindingRap guanine nucleotide exchange factor 3Homo sapiens (human)
protein domain specific bindingRap guanine nucleotide exchange factor 3Homo sapiens (human)
cAMP bindingRap guanine nucleotide exchange factor 3Homo sapiens (human)
nucleoside bindingCytidine deaminaseHomo sapiens (human)
cytidine deaminase activityCytidine deaminaseHomo sapiens (human)
protein bindingCytidine deaminaseHomo sapiens (human)
zinc ion bindingCytidine deaminaseHomo sapiens (human)
identical protein bindingCytidine deaminaseHomo sapiens (human)
protein homodimerization activityCytidine deaminaseHomo sapiens (human)
neurotransmitter transmembrane transporter activityEquilibrative nucleoside transporter 2Homo sapiens (human)
nucleoside transmembrane transporter activityEquilibrative nucleoside transporter 2Homo sapiens (human)
nucleobase transmembrane transporter activityEquilibrative nucleoside transporter 2Homo sapiens (human)
adenine transmembrane transporter activityEquilibrative nucleoside transporter 2Homo sapiens (human)
guanine transmembrane transporter activityEquilibrative nucleoside transporter 2Homo sapiens (human)
uracil transmembrane transporter activityEquilibrative nucleoside transporter 2Homo sapiens (human)
purine nucleoside transmembrane transporter activityEquilibrative nucleoside transporter 2Homo sapiens (human)
cytidine transmembrane transporter activityEquilibrative nucleoside transporter 2Homo sapiens (human)
uridine transmembrane transporter activityEquilibrative nucleoside transporter 2Homo sapiens (human)
protein bindingProtein cereblonHomo sapiens (human)
transmembrane transporter bindingProtein cereblonHomo sapiens (human)
metal ion bindingProtein cereblonHomo sapiens (human)
neurotransmitter transmembrane transporter activityEquilibrative nucleoside transporter 1Homo sapiens (human)
nucleoside transmembrane transporter activityEquilibrative nucleoside transporter 1Homo sapiens (human)
adenine transmembrane transporter activityEquilibrative nucleoside transporter 1Homo sapiens (human)
guanine transmembrane transporter activityEquilibrative nucleoside transporter 1Homo sapiens (human)
uracil transmembrane transporter activityEquilibrative nucleoside transporter 1Homo sapiens (human)
purine nucleoside transmembrane transporter activityEquilibrative nucleoside transporter 1Homo sapiens (human)
cytidine transmembrane transporter activityEquilibrative nucleoside transporter 1Homo sapiens (human)
uridine transmembrane transporter activityEquilibrative nucleoside transporter 1Homo sapiens (human)
pyrimidine- and adenosine-specific:sodium symporter activityEquilibrative nucleoside transporter 1Homo sapiens (human)
uridine kinase activityUridine-cytidine kinase 1 Homo sapiens (human)
ATP bindingUridine-cytidine kinase 1 Homo sapiens (human)
cytidine kinase activityUridine-cytidine kinase 1 Homo sapiens (human)
purine nucleobase transmembrane transporter activitySolute carrier family 28 member 3Homo sapiens (human)
nucleoside:sodium symporter activitySolute carrier family 28 member 3Homo sapiens (human)
protein bindingSolute carrier family 28 member 3Homo sapiens (human)
uridine transmembrane transporter activitySolute carrier family 28 member 3Homo sapiens (human)
purine-specific nucleoside:sodium symporter activitySolute carrier family 28 member 3Homo sapiens (human)
pyrimidine- and adenosine-specific:sodium symporter activitySolute carrier family 28 member 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (28)

Processvia Protein(s)Taxonomy
cytosolSodium/nucleoside cotransporter 1Homo sapiens (human)
plasma membraneSodium/nucleoside cotransporter 1Homo sapiens (human)
apical plasma membraneSodium/nucleoside cotransporter 1Homo sapiens (human)
nuclear speckSodium/nucleoside cotransporter 1Homo sapiens (human)
brush border membraneSodium/nucleoside cotransporter 1Homo sapiens (human)
plasma membraneSodium/nucleoside cotransporter 1Homo sapiens (human)
plasma membraneSodium/nucleoside cotransporter 2Homo sapiens (human)
vesicle membraneSodium/nucleoside cotransporter 2Homo sapiens (human)
membraneSodium/nucleoside cotransporter 2Homo sapiens (human)
apicolateral plasma membraneSodium/nucleoside cotransporter 2Homo sapiens (human)
coated vesicleSodium/nucleoside cotransporter 2Homo sapiens (human)
brush border membraneSodium/nucleoside cotransporter 2Homo sapiens (human)
plasma membraneSodium/nucleoside cotransporter 2Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 3Homo sapiens (human)
cortical actin cytoskeletonRap guanine nucleotide exchange factor 3Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 3Homo sapiens (human)
microvillusRap guanine nucleotide exchange factor 3Homo sapiens (human)
endomembrane systemRap guanine nucleotide exchange factor 3Homo sapiens (human)
membraneRap guanine nucleotide exchange factor 3Homo sapiens (human)
lamellipodiumRap guanine nucleotide exchange factor 3Homo sapiens (human)
filopodiumRap guanine nucleotide exchange factor 3Homo sapiens (human)
extracellular exosomeRap guanine nucleotide exchange factor 3Homo sapiens (human)
extracellular regionCytidine deaminaseHomo sapiens (human)
cytosolCytidine deaminaseHomo sapiens (human)
secretory granule lumenCytidine deaminaseHomo sapiens (human)
tertiary granule lumenCytidine deaminaseHomo sapiens (human)
ficolin-1-rich granule lumenCytidine deaminaseHomo sapiens (human)
cytosolCytidine deaminaseHomo sapiens (human)
nucleolusEquilibrative nucleoside transporter 2Homo sapiens (human)
plasma membraneEquilibrative nucleoside transporter 2Homo sapiens (human)
basolateral plasma membraneEquilibrative nucleoside transporter 2Homo sapiens (human)
apical plasma membraneEquilibrative nucleoside transporter 2Homo sapiens (human)
basolateral plasma membraneEquilibrative nucleoside transporter 2Homo sapiens (human)
plasma membraneEquilibrative nucleoside transporter 2Homo sapiens (human)
nucleusProtein cereblonHomo sapiens (human)
cytoplasmProtein cereblonHomo sapiens (human)
cytosolProtein cereblonHomo sapiens (human)
membraneProtein cereblonHomo sapiens (human)
perinuclear region of cytoplasmProtein cereblonHomo sapiens (human)
Cul4A-RING E3 ubiquitin ligase complexProtein cereblonHomo sapiens (human)
plasma membraneEquilibrative nucleoside transporter 1Homo sapiens (human)
membraneEquilibrative nucleoside transporter 1Homo sapiens (human)
basolateral plasma membraneEquilibrative nucleoside transporter 1Homo sapiens (human)
apical plasma membraneEquilibrative nucleoside transporter 1Homo sapiens (human)
presynapseEquilibrative nucleoside transporter 1Homo sapiens (human)
postsynapseEquilibrative nucleoside transporter 1Homo sapiens (human)
plasma membraneEquilibrative nucleoside transporter 1Homo sapiens (human)
cytosolUridine-cytidine kinase 1 Homo sapiens (human)
cytoplasmUridine-cytidine kinase 1 Homo sapiens (human)
endoplasmic reticulum membraneSolute carrier family 28 member 3Homo sapiens (human)
plasma membraneSolute carrier family 28 member 3Homo sapiens (human)
brush border membraneSolute carrier family 28 member 3Homo sapiens (human)
plasma membraneSolute carrier family 28 member 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (79)

Assay IDTitleYearJournalArticle
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1222905Binding affinity to recombinant human ENT1 expressed in Saccharomyces cerevisiae assessed as inhibition of [3H]-uridine transport after 15 mins by scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Transport of A1 adenosine receptor agonist tecadenoson by human and mouse nucleoside transporters: evidence for blood-brain barrier transport by murine equilibrative nucleoside transporter 1 mENT1.
AID1879226Antiviral activity against HCV by replicon assay2022Bioorganic & medicinal chemistry letters, 04-01, Volume: 61Design, chemical synthesis and antiviral evaluation of 2'-deoxy-2'-fluoro-2'-C-methyl-4'-thionucleosides.
AID1222918Drug transport in Xenopus laevis oocytes assessed as recombinant human CNT3-mediated uptake by measuring induction of sodium currents at 100 to 500 uM by electrophysiological method2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Transport of A1 adenosine receptor agonist tecadenoson by human and mouse nucleoside transporters: evidence for blood-brain barrier transport by murine equilibrative nucleoside transporter 1 mENT1.
AID1467207Antiinflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced NO production pretreated for 30 mins followed by LPS stimulation for 24 hrs by Griess assay2017Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12
Alkaloids from aerial parts of Houttuynia cordata and their anti-inflammatory activity.
AID332709Antiviral activity against HIV1 3B infected in human H9 cells after 4 days by p24 antigen ELISA assay1995Journal of natural products, Mar, Volume: 58, Issue:3
Anti-AIDS agents, 18. Sodium and potassium salts of caffeic acid tetramers from Arnebia euchroma as anti-HIV agents.
AID1222909Binding affinity to recombinant human CNT3 expressed in Saccharomyces cerevisiae assessed as inhibition of [3H]-uridine transport after 5 mins by scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Transport of A1 adenosine receptor agonist tecadenoson by human and mouse nucleoside transporters: evidence for blood-brain barrier transport by murine equilibrative nucleoside transporter 1 mENT1.
AID453747Inhibition of Escherichia coli recombinant N-terminal hexahistidine-tagged CTP synthetase expressed in Escherichia coli BL21 (DE3) assessed as inhibition of CTP formation by continuous spectrophotometric assay in presence of 10 mM L-glutamine and 0.15 mM 2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Inhibition of CTP synthase from Escherichia coli by xanthines and uric acids.
AID278936Activity of human UCK1 expressed in Huh7 cells assessed as phosphorylation by coupled enzyme assay2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Mechanism of activation of beta-D-2'-deoxy-2'-fluoro-2'-c-methylcytidine and inhibition of hepatitis C virus NS5B RNA polymerase.
AID381854Activity of Escherichia coli thymidine phosphorylase assessed as drug phosphorylation after 2 hrs2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Kinetic parameters and recognition of thymidine analogues with varying functional groups by thymidine phosphorylase.
AID140060Tested for PB (pentobarbital)-induced sleep effect expressed as percent control of sleeping time at a dosage (icv) of 1.0 uM concentration1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
N-substituted oxopyrimidines and nucleosides: structure-activity relationship for hypnotic activity as central nervous system depressant.
AID28713Partition coefficient (logP)1992Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12
Chemistry and anti-HIV properties of 2'-fluoro-2',3'-dideoxyarabinofuranosylpyrimidines.
AID1054097Half life in mouse plasma2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Design of novel potent inhibitors of human uridine phosphorylase-1: synthesis, inhibition studies, thermodynamics, and in vitro influence on 5-fluorouracil cytotoxicity.
AID1136938Non-competitive inhibition of Escherichia coli B thymidine kinase using [2-14C]-thymidine as substrate assessed as formation of [14C]-TMP after 10 mins by Lineweaver-Burk double reciprocal plot analysis1979Journal of medicinal chemistry, Dec, Volume: 22, Issue:12
Design of species- or isozyme-specific enzyme inhibitors. 2. Differences between a bacterial and a mammalian thymidine kinase in the effect of thymidine substituents on affinity for the thymidine site.
AID140062Tested for PB (pentobarbital)-induced sleep effect expressed as percent control of sleeping time at a dosage (icv) of 2.4 uM concentration1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
N-substituted oxopyrimidines and nucleosides: structure-activity relationship for hypnotic activity as central nervous system depressant.
AID1222916Drug transport in Xenopus laevis oocytes assessed as recombinant human CNT1-mediated uptake by measuring induction of sodium currents at 100 to 500 uM by electrophysiological method2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Transport of A1 adenosine receptor agonist tecadenoson by human and mouse nucleoside transporters: evidence for blood-brain barrier transport by murine equilibrative nucleoside transporter 1 mENT1.
AID381860Activity of Escherichia coli thymidine phosphorylase assessed as drug phosphorylation after 1 hr2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Kinetic parameters and recognition of thymidine analogues with varying functional groups by thymidine phosphorylase.
AID55389Compound was tested for its binding affinity against cytidine deaminase.1998Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
Carbocyclic analogues of the potent cytidine deaminase inhibitor 1-(beta-D-ribofuranosyl)-1,2-dihydropyrimidin-2-one (zebularine).
AID278937Ratio of Kcat to Km for UCK1 activity expressed in Huh7 cells2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Mechanism of activation of beta-D-2'-deoxy-2'-fluoro-2'-c-methylcytidine and inhibition of hepatitis C virus NS5B RNA polymerase.
AID718193Competitive inhibition of bovine pancreatic RNase A type 12-A assessed as degradation of yeast tRNA preincubated for 10 mins before addition of the enzyme by double reciprocal plot analysis2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Triazole pyrimidine nucleosides as inhibitors of Ribonuclease A. Synthesis, biochemical, and structural evaluation.
AID210890Ability to inhibit rat cytoplasmic Thymidine kinase1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Species- or isozyme-specific enzyme inhibitors. 5. Differential effects of thymidine substituents on affinity for rat thymidine kinase isozymes.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID140063Tested for PB (pentobarbital)-induced sleep effect expressed as percent control of sleeping time at a dosage (icv) of 3.8 uM concentration1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
N-substituted oxopyrimidines and nucleosides: structure-activity relationship for hypnotic activity as central nervous system depressant.
AID1222907Binding affinity to recombinant human CNT1 expressed in Saccharomyces cerevisiae assessed as inhibition of [3H]-uridine transport after 15 mins by scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Transport of A1 adenosine receptor agonist tecadenoson by human and mouse nucleoside transporters: evidence for blood-brain barrier transport by murine equilibrative nucleoside transporter 1 mENT1.
AID126601Ability to inhibit rat mitochondrial thymidine kinase1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Species- or isozyme-specific enzyme inhibitors. 5. Differential effects of thymidine substituents on affinity for rat thymidine kinase isozymes.
AID332711Therapeutic index, ratio of IC50 for human H9 cells to EC50 for HIV1 3B1995Journal of natural products, Mar, Volume: 58, Issue:3
Anti-AIDS agents, 18. Sodium and potassium salts of caffeic acid tetramers from Arnebia euchroma as anti-HIV agents.
AID96814In vitro inhibitory activity against growth of L1210 mouse leukemia cells at 10E-4 M concentration; IA means Inactive1982Journal of medicinal chemistry, Jul, Volume: 25, Issue:7
Synthesis of pyridazine analogues of the naturally occurring nucleosides cytidine, uridine, deoxycytidine, and deoxyuridine.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1766075Cytotoxicity against in mouse 3T3-L1 cells assessed as reduction in cell viability at 100 uM incubated for 24 hrs by MTT assay relative to control2021Bioorganic & medicinal chemistry letters, 10-01, Volume: 49Phytochemicals from the flowers of Prunus persica (L.) Batsch: Anti-adipogenic effect of mandelamide on 3T3-L1 preadipocytes.
AID1054094Induction of uridine phosphorylase-mediated drug metabolism in rat liver2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Design of novel potent inhibitors of human uridine phosphorylase-1: synthesis, inhibition studies, thermodynamics, and in vitro influence on 5-fluorouracil cytotoxicity.
AID1685005Binding affinity to human CRBN-thalidomide binding domain expressed in Escherichia coli by measuring baseline corrected normalized fluorescence by MST based assay2021ACS medicinal chemistry letters, Jan-14, Volume: 12, Issue:1
Sweet and Blind Spots in E3 Ligase Ligand Space Revealed by a Thermophoresis-Based Assay.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID717236Binding affinity to Streptomyces avidinii streptavidin at 4 mM using dye labeled Streptavidin binding aptamer by fluorescence spectral analysis method2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Specific interactions between adenosine and streptavidin/avidin.
AID1222908Binding affinity to recombinant human CNT2 expressed in Saccharomyces cerevisiae assessed as inhibition of [3H]-uridine transport after 15 mins by scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Transport of A1 adenosine receptor agonist tecadenoson by human and mouse nucleoside transporters: evidence for blood-brain barrier transport by murine equilibrative nucleoside transporter 1 mENT1.
AID399372Deterrent activity against Perknaster fuscus assessed as induction of sustained retractions of tube-feet by sea-star deterrent assay1998Journal of natural products, Jan, Volume: 61, Issue:1
Purine and nucleoside metabolites from the Antarctic sponge Isodictya erinacea.
AID123967Hypnotic activity expressed as sleeping time was determined in ddN strain mice by the icv administration of 3.8 uMol/mouse of the compound; None indicates that the mouse could not fall into sleep1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
N-substituted oxopyrimidines and nucleosides: structure-activity relationship for hypnotic activity as central nervous system depressant.
AID1659751Agonist activity at TRPA1 (unknown origin) at 1000 uM relative to AITC2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Identification of a new class of non-electrophilic TRPA1 agonists by a structure-based virtual screening approach.
AID97414In vivo percent increase in life span (%ILS) of mice bearing L1210 leukemia at a dose of 400 mg/kg1982Journal of medicinal chemistry, Jul, Volume: 25, Issue:7
Synthesis of pyridazine analogues of the naturally occurring nucleosides cytidine, uridine, deoxycytidine, and deoxyuridine.
AID97848The concentration required (hypoxanthine+uridine) to inhibit the growth of L-1210 leukemic cells was evaluated1985Journal of medicinal chemistry, Apr, Volume: 28, Issue:4
Synthesis and biological activity of a novel adenosine analogue, 3-beta-D-ribofuranosylthieno[2,3-d]pyrimidin-4-one.
AID453744Inhibition of Escherichia coli recombinant N-terminal hexahistidine-tagged CTP synthetase expressed in Escherichia coli BL21 (DE3) assessed as inhibition of CTP formation by continuous spectrophotometric assay in presence of 150 mM NH4Cl2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Inhibition of CTP synthase from Escherichia coli by xanthines and uric acids.
AID201571Phosphorylation by uridine/cytidine kinase(UCK) from mouse sarcoma -180 ascites cells was measured.1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Nucleosides and nucleotides. 175. Structural requirements of the sugar moiety for the antitumor activities of new nucleoside antimetabolites, 1-(3-C-ethynyl-beta-D-ribo-pentofuranosyl)cytosine and -uracil1.
AID97844The concentration required to inhibit the growth of L-1210 leukemic cells was evaluated; 1E-3 to 1E-41985Journal of medicinal chemistry, Apr, Volume: 28, Issue:4
Synthesis and biological activity of a novel adenosine analogue, 3-beta-D-ribofuranosylthieno[2,3-d]pyrimidin-4-one.
AID123974Hypnotic activity in ddN strain mice by the iv administration of 0.5 mmol/kg; No activity.1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
N-substituted oxopyrimidines and nucleosides: structure-activity relationship for hypnotic activity as central nervous system depressant.
AID427711Inhibition of NADH oxidase in beef heart submitochondrial particles by end-window spectrophotometry2009Journal of natural products, Jul, Volume: 72, Issue:7
Terretonins E and F, inhibitors of the mitochondrial respiratory chain from the marine-derived fungus Aspergillus insuetus (#).
AID1222906Binding affinity to recombinant human ENT2 expressed in Saccharomyces cerevisiae assessed as inhibition of [3H]-uridine transport after 15 mins by scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Transport of A1 adenosine receptor agonist tecadenoson by human and mouse nucleoside transporters: evidence for blood-brain barrier transport by murine equilibrative nucleoside transporter 1 mENT1.
AID1766076Inhibition of preadipocyte differentiation in mouse 3T3-L1 cells assessed as lipid droplet accumulation at 100 uM incubated for 8 days by Oil Red O staining method relative to untreated control2021Bioorganic & medicinal chemistry letters, 10-01, Volume: 49Phytochemicals from the flowers of Prunus persica (L.) Batsch: Anti-adipogenic effect of mandelamide on 3T3-L1 preadipocytes.
AID1222917Drug transport in Xenopus laevis oocytes assessed as recombinant human CNT2-mediated uptake by measuring induction of sodium currents at 100 to 500 uM by electrophysiological method2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Transport of A1 adenosine receptor agonist tecadenoson by human and mouse nucleoside transporters: evidence for blood-brain barrier transport by murine equilibrative nucleoside transporter 1 mENT1.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1811Experimentally measured binding affinity data derived from PDB1997Biochemistry, Apr-22, Volume: 36, Issue:16
The structure of the cytidine deaminase-product complex provides evidence for efficient proton transfer and ground-state destabilization.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB1997Biochemistry, Apr-22, Volume: 36, Issue:16
The structure of the cytidine deaminase-product complex provides evidence for efficient proton transfer and ground-state destabilization.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2013PloS one, , Volume: 8, Issue:7
The mode of inhibitor binding to peptidyl-tRNA hydrolase: binding studies and structure determination of unbound and bound peptidyl-tRNA hydrolase from Acinetobacter baumannii.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2014eLife, Jul-31, Volume: 3Structural basis of nucleoside and nucleoside drug selectivity by concentrative nucleoside transporters.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12,266)

TimeframeStudies, This Drug (%)All Drugs %
pre-19909071 (73.95)18.7374
1990's977 (7.97)18.2507
2000's1038 (8.46)29.6817
2010's874 (7.13)24.3611
2020's306 (2.49)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 45.93

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index45.93 (24.57)
Research Supply Index9.46 (2.92)
Research Growth Index4.39 (4.65)
Search Engine Demand Index118.54 (26.88)
Search Engine Supply Index2.94 (0.95)

This Compound (45.93)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials69 (0.54%)5.53%
Reviews264 (2.07%)6.00%
Case Studies52 (0.41%)4.05%
Observational1 (0.01%)0.25%
Other12,363 (96.97%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]