Page last updated: 2024-11-04

pteridines

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID1043
CHEBI ID27601
SCHEMBL ID7626
MeSH IDM0018072

Synonyms (29)

Synonym
1,3,5,8-tetraazanaphthalene
CHEBI:27601
pyrimido[4,5-b]pyrazine
1,5,8-tetraazanaphthalene
azinepurine
nsc-268562
nsc268562
pyrazino[2,3-d]pyrimidine
inchi=1/c6h4n4/c1-2-9-6-5(8-1)3-7-4-10-6/h1-4
pteridene
91-18-9
PTERIDINE-RING
pteridine
C07581
pteridines ,
AKOS006305842
FT-0685162
unii-6ezf26xq81
6ezf26xq81 ,
pyrimido(4,5-b)pyrazine
pyrazino(2,3-d)pyrimidine
nsc 268562
pteridine [mi]
SCHEMBL7626
DTXSID60238347
pteridine (6ci,7ci,8ci,9ci)
Q414021
AMY15887
CS-0362609

Research Excerpts

Overview

Pteridines are a class of compounds excreted in urine, the levels of which are found to elevate significantly in tumor-related diseases. Pteridine concentrations may be increased in some disorders, such as infections, autoimmune disorders and cancer.

ExcerptReferenceRelevance
"Pteridines are an important class of fused heterocycles found in natural products and drug molecules, and have shown diverse biological activities. "( Design, synthesis and preliminary biological evaluation of 5,8-dihydropteridine-6,7-diones that induce apoptosis and suppress cell migration.
Fu, DJ; Geng, PF; Hu, XN; Li, ZH; Liu, HM; Wang, CC; Yu, B; Zhao, B; Zhao, TQ, 2018
)
1.92
"Pteridines are a group of endogenous heterocyclic compounds whose concentrations in biological fluids may be increased in some disorders, such as infections, autoimmune disorders and cancer. "( Determination of pteridines in biological samples with an emphasis on their stability.
Nováková, L; Solich, P; Tomšík, P; Tomšíková, H, 2013
)
2.17
"Pteridines are a diverse family of endogenous metabolites that may serve as useful diagnostic biomarkers for disease. "( High-throughput intracellular pteridinic profiling by liquid chromatography-quadrupole time-of-flight mass spectrometry.
Bai, Y; Burton, C; Liu, H; Ma, Y; Weng, R; Yang, L, 2015
)
1.86
"Pteridines are a class of potential cancer biomarkers."( Metabolic profiling of pteridines for determination of potential biomarkers in cancer diseases.
Bujak, R; Daghir, E; Kośliński, P; Markuszewski, MJ, 2011
)
1.4
"Pteridines are a class of compounds excreted in urine, the levels of which are found to elevate significantly in tumor-related diseases. "( Pteridine analysis in urine by capillary electrophoresis using laser-induced fluorescence detection.
Han, F; Huynh, BH; Lin, B; Ma, Y; Shi, H, 1999
)
1.75

Toxicity

ExcerptReferenceRelevance
" coli) by these toxic agents and its modulation by neopterin and 7,8-dihydroneopterin."( Neopterin derivatives modulate toxicity of reactive species on Escherichia coli.
Fuchs, D; Wede, I; Widner, B, 1999
)
0.3
" Tetrahydrobiopterin, an essential cofactor for tyrosine hydroxylase, may act as an antioxidant in dopaminergic neurones and protects against the toxic consequences of glutathione depletion."( Tetrahydrobiopterin precursor sepiapterin provides protection against neurotoxicity of 1-methyl-4-phenylpyridinium in nigral slice cultures.
Gramsbergen, JB; Hesslinger, C; Jansen, P; Madsen, JT; Meyer, M; Zimmer, J, 2003
)
0.32
" Grade 4 neutropenia occurred in 37% of patients; common nonhematologic adverse events were fatigue (31%) and nausea (27%)."( The efficacy and safety of BI 2536, a novel Plk-1 inhibitor, in patients with stage IIIB/IV non-small cell lung cancer who had relapsed after, or failed, chemotherapy: results from an open-label, randomized phase II clinical trial.
Frickhofen, N; Fritsch, H; Gaschler-Markefski, B; Hanft, G; Kortsik, C; Munzert, G; Reck, M; Schuler, M; Sebastian, M; von Pawel, J; Waller, CF, 2010
)
0.36
" Minimal treatment-related adverse events were seen at doses up to 8 mg."( Safety, pharmacokinetics and pharmacodynamics of GS-9620, an oral Toll-like receptor 7 agonist.
Frey, CR; Hesselgesser, J; Kearney, B; Lopatin, U; McHutchison, JG; Moorehead, L; Ohmstede, C; Subramanian, GM; Tumas, D; Wolfgang, G, 2013
)
0.39
" Pharmacodynamic activity is seen before adverse events, suggesting the potential for induction of an antiviral response without systemic adverse events in subjects with chronic viral hepatitis."( Safety, pharmacokinetics and pharmacodynamics of GS-9620, an oral Toll-like receptor 7 agonist.
Frey, CR; Hesselgesser, J; Kearney, B; Lopatin, U; McHutchison, JG; Moorehead, L; Ohmstede, C; Subramanian, GM; Tumas, D; Wolfgang, G, 2013
)
0.39
" In healthy volunteers, low doses of GS-9620 (2, 4 and 6 mg) induced significant expression of peripheral interferon-stimulated-gene (ISG) mRNA in the absence of detectable serum interferon-α and systemic adverse events (AEs)."( Safety, pharmacokinetics and pharmacodynamics of the oral toll-like receptor 7 agonist GS-9620 in treatment-naive patients with chronic hepatitis C.
Freilich, B; Gaggar, A; Gruener, D; Hassman, D; Hill, J; Jacobson, IM; Lawitz, E; Marbury, T; Massetto, B; McHutchison, JG; Mogalian, E; Nguyen, AH; Pflanz, S; Rodriguez-Torres, M; Subramanian, GM; Webster, L, 2015
)
0.42
"Vesatolimod was safe and well-tolerated in patients with CHB, demonstrating consistent dose-dependent pharmacodynamic induction of ISG15 without significant systemic induction of IFNα expression or related symptoms."( Safety, efficacy and pharmacodynamics of vesatolimod (GS-9620) in virally suppressed patients with chronic hepatitis B.
Ahn, SH; Brunetto, MR; Ferrari, C; Fung, S; Gaggar, A; Gane, EJ; Janssen, HLA; Joshi, A; Kim, YJ; Lau, AH; Massetto, B; Nguyen, AH; Subramanian, GM; Tsai, NCS; Woo, J; Yoshida, EM, 2018
)
0.48
"In a phase II study, vesatolimod, an oral, once-weekly, experimental immune-activating drug for the treatment of hepatitis B virus (HBV), is safe and well-tolerated in chronic HBV patients who are virally suppressed on oral antiviral treatment."( Safety, efficacy and pharmacodynamics of vesatolimod (GS-9620) in virally suppressed patients with chronic hepatitis B.
Ahn, SH; Brunetto, MR; Ferrari, C; Fung, S; Gaggar, A; Gane, EJ; Janssen, HLA; Joshi, A; Kim, YJ; Lau, AH; Massetto, B; Nguyen, AH; Subramanian, GM; Tsai, NCS; Woo, J; Yoshida, EM, 2018
)
0.48
"1%) experienced ≥1 treatment-emergent adverse event; the majority were mild or moderate in severity."( Safety and efficacy of vesatolimod (GS-9620) in patients with chronic hepatitis B who are not currently on antiviral treatment.
Agarwal, K; Ahn, SH; Andreone, P; Bulusu, A; Cathcart, AL; Chuang, WL; Elkhashab, M; Gaggar, A; Kim, HJ; Lau, AH; Nguyen, MH; Subramanian, GM; Tian, X; Woo, J, 2018
)
0.48

Pharmacokinetics

ExcerptReferenceRelevance
"The MTD of BI 2536 when administered as a single-dose, 1-hour infusion was 200 mg; BI 2536 was well tolerated and showed a favorable pharmacokinetic profile."( Phase I dose escalation and pharmacokinetic study of BI 2536, a novel Polo-like kinase 1 inhibitor, in patients with advanced solid tumors.
Frost, A; Hedbom, S; Hoesl, CE; Kaiser, R; Mross, K; Munzert, G; Rentschler, J; Rouyrre, N; Steinbild, S; Trommeshauser, D, 2008
)
0.35
"GS-9620 demonstrates safety and pharmacodynamic activity at doses up to 12 mg."( Safety, pharmacokinetics and pharmacodynamics of GS-9620, an oral Toll-like receptor 7 agonist.
Frey, CR; Hesselgesser, J; Kearney, B; Lopatin, U; McHutchison, JG; Moorehead, L; Ohmstede, C; Subramanian, GM; Tumas, D; Wolfgang, G, 2013
)
0.39
" We characterized the pharmacodynamic response of GS-9620 in CD-1 mice and cynomolgus monkeys following intravenous or oral administration and showed that GS-9620 induces the production of select chemokines and cytokines, including IFN-α and interferon-stimulated genes (ISGs)."( Pharmacokinetic and pharmacodynamic properties of GS-9620, a novel Toll-like receptor 7 agonist, demonstrate interferon-stimulated gene induction without detectable serum interferon at low oral doses.
Fosdick, A; Frey, CR; Halcomb, RL; Hesselgesser, J; Pflanz, S; Tumas, DB; Wolfgang, G; Zheng, J, 2014
)
0.4
" Pharmacodynamic assessments included peripheral ISG15 mRNA expression, serum interferon-α and interferon-γ-inducible protein (IP)-10 levels and HCV RNA quantification."( Safety, pharmacokinetics and pharmacodynamics of the oral toll-like receptor 7 agonist GS-9620 in treatment-naive patients with chronic hepatitis C.
Freilich, B; Gaggar, A; Gruener, D; Hassman, D; Hill, J; Jacobson, IM; Lawitz, E; Marbury, T; Massetto, B; McHutchison, JG; Mogalian, E; Nguyen, AH; Pflanz, S; Rodriguez-Torres, M; Subramanian, GM; Webster, L, 2015
)
0.42
" Finally, volasertib and cytarabine did not influence the pharmacokinetic characteristics of each other."( Population Pharmacokinetics of Volasertib Administered in Patients with Acute Myeloid Leukaemia as a Single Agent or in Combination with Cytarabine.
Fleury, A; Freiwald, M; Fritsch, H; Haug, K; P Solans, B; Trocóniz, IF, 2018
)
0.48
"Vesatolimod was safe and well-tolerated in patients with CHB, demonstrating consistent dose-dependent pharmacodynamic induction of ISG15 without significant systemic induction of IFNα expression or related symptoms."( Safety, efficacy and pharmacodynamics of vesatolimod (GS-9620) in virally suppressed patients with chronic hepatitis B.
Ahn, SH; Brunetto, MR; Ferrari, C; Fung, S; Gaggar, A; Gane, EJ; Janssen, HLA; Joshi, A; Kim, YJ; Lau, AH; Massetto, B; Nguyen, AH; Subramanian, GM; Tsai, NCS; Woo, J; Yoshida, EM, 2018
)
0.48

Compound-Compound Interactions

ExcerptReferenceRelevance
" Most importantly, the administration of BI-2536, in combination with doxorubicin + cyclophosphamide chemotherapy, led to a faster complete response compared with the chemotherapy treatment alone and prevented relapse, which is the major risk associated with TNBC."( Polo-like kinase 1: a potential therapeutic option in combination with conventional chemotherapy for the management of patients with triple-negative breast cancer.
Barillot, E; Cruzalegui, F; De Koning, L; Decaudin, D; Depil, S; Dubois, T; Dumont, A; Gentien, D; Gravier, E; Lang, G; Maire, V; Marangoni, E; Marty-Prouvost, B; Némati, F; Pierré, A; Richardson, M; Rigaill, G; Roman-Roman, S; Tesson, B; Tucker, GC; Vincent-Salomon, A, 2013
)
0.39
" Therefore, we studied the effect of polo-like kinase 1 (Plk1) inhibitors on prostate cancer cells as a single agent and in combination with histone deacetylase (HDAC) inhibitors valproic acid and vorinostat."( Targeting prostate cancer cell lines with polo-like kinase 1 inhibitors as a single agent and in combination with histone deacetylase inhibitors.
Carducci, MA; Gonzalez, M; Hammers, H; Kachhap, SK; Kaelber, NS; Kim, E; Kortenhorst, MS; Mendonca, J; van Diest, PJ; Wissing, MD, 2013
)
0.39
" In this study, we tested the second-generation PLK1 inhibitors BI 6727 and GSK461364 in HOS and MG-63 cell lines, both as a single agent and in combination with methotrexate, cisplatin, vinblastine, doxorubicin, or ionizing radiation."( BI 6727 and GSK461364 suppress growth and radiosensitize osteosarcoma cells, but show limited cytotoxic effects when combined with conventional treatments.
Bogado, RF; Brassesco, MS; de Oliveira, HF; Pezuk, JA; Tone, LG, 2015
)
0.42
" This randomized, phase II trial (n [ 143) investigated volasertib monotherapy or in combination with pemetrexed compared with pemetrexed monotherapy in patients with NSCLC whose disease had progressed after previous platinum-based chemotherapy."( A Randomized, Open-Label Phase II Trial of Volasertib as Monotherapy and in Combination With Standard-Dose Pemetrexed Compared With Pemetrexed Monotherapy in Second-Line Treatment for Non-Small-Cell Lung Cancer.
Blais, N; Chu, Q; Ellis, PM; Gu, Y; Hirsh, V; Leighl, NB; Liu, D; Pilz, K; Reaume, MN; Sadrolhefazi, B; Wierzbicki, R, 2015
)
0.42
" Pharmacokinetics analyses showed no drug-drug interactions between volasertib and pemetrexed."( A Randomized, Open-Label Phase II Trial of Volasertib as Monotherapy and in Combination With Standard-Dose Pemetrexed Compared With Pemetrexed Monotherapy in Second-Line Treatment for Non-Small-Cell Lung Cancer.
Blais, N; Chu, Q; Ellis, PM; Gu, Y; Hirsh, V; Leighl, NB; Liu, D; Pilz, K; Reaume, MN; Sadrolhefazi, B; Wierzbicki, R, 2015
)
0.42
"To determine the maximum tolerated dose (MTD) of volasertib, a Polo-like kinase inhibitor, combined with afatinib, an oral irreversible ErbB family blocker, in patients with advanced solid tumors (NCT01206816; Study 1230."( A phase I study of volasertib combined with afatinib, in advanced solid tumors.
De Smet, M; Herremans, C; Liu, D; Machiels, JP; Peeters, M; Pilz, K; Rottey, S; Specenier, P; Strelkowa, N; Surmont, V, 2015
)
0.42
"Patients with advanced non-resectable and/or metastatic disease following failure of conventional treatment received intravenous volasertib 150-300 mg on day 1 every 21 days, combined with oral afatinib 30-40 mg on days 2-21 of a 3-week cycle (Schedule A), or 50-90 mg on days 2-6 of a 3-week cycle (Schedule B)."( A phase I study of volasertib combined with afatinib, in advanced solid tumors.
De Smet, M; Herremans, C; Liu, D; Machiels, JP; Peeters, M; Pilz, K; Rottey, S; Specenier, P; Strelkowa, N; Surmont, V, 2015
)
0.42
"Volasertib combined with afatinib had manageable adverse effects and limited antitumor activity in this heavily pretreated population."( A phase I study of volasertib combined with afatinib, in advanced solid tumors.
De Smet, M; Herremans, C; Liu, D; Machiels, JP; Peeters, M; Pilz, K; Rottey, S; Specenier, P; Strelkowa, N; Surmont, V, 2015
)
0.42
" This study determined the maximum tolerated dose (MTD) and pharmacokinetics of volasertib combined with nintedanib, a potent and orally bioavailable triple angiokinase inhibitor, in patients with advanced solid tumors."( A phase I, dose-escalation study of volasertib combined with nintedanib in advanced solid tumors.
Cascinu, S; Clementi, L; de Braud, F; De Pas, T; Liu, D; Pilz, K; Sikken, P; Spitaleri, G, 2015
)
0.42
" The primary objective was the MTD of volasertib in combination with nintedanib."( A phase I, dose-escalation study of volasertib combined with nintedanib in advanced solid tumors.
Cascinu, S; Clementi, L; de Braud, F; De Pas, T; Liu, D; Pilz, K; Sikken, P; Spitaleri, G, 2015
)
0.42
"Volasertib could be combined with fixed-dose nintedanib at the recommended single-agent dose."( A phase I, dose-escalation study of volasertib combined with nintedanib in advanced solid tumors.
Cascinu, S; Clementi, L; de Braud, F; De Pas, T; Liu, D; Pilz, K; Sikken, P; Spitaleri, G, 2015
)
0.42
"Volasertib, a potent and selective polo-like kinase inhibitor, has shown to increase response rates and improve survival with a clinically manageable safety profile, administered alone and in combination with cytarabine in patients with acute myeloid leukaemia."( Population Pharmacokinetics of Volasertib Administered in Patients with Acute Myeloid Leukaemia as a Single Agent or in Combination with Cytarabine.
Fleury, A; Freiwald, M; Fritsch, H; Haug, K; P Solans, B; Trocóniz, IF, 2018
)
0.48
"The pharmacokinetics of volasertib in patients with acute myeloid leukaemia alone or in combination with cytarabine is predictable and associated with low-to-mild patient variability with the exception of the high variability associated with the volume of distribution of the central compartment, having no effect on the area under the plasma concentration-time curve."( Population Pharmacokinetics of Volasertib Administered in Patients with Acute Myeloid Leukaemia as a Single Agent or in Combination with Cytarabine.
Fleury, A; Freiwald, M; Fritsch, H; Haug, K; P Solans, B; Trocóniz, IF, 2018
)
0.48
" Herein, we investigated the in vitro effects of two second-generation PLK1 inhibitors BI 6727 and GSK461364 in breast cancer cell lines as monotherapy or in combination with other drugs or ionizing radiation."( PLK1 Inhibition Radiosensitizes Breast Cancer Cells, but Shows Low Efficacy as Monotherapy or in Combination with other Cytotoxic Drugs.
Brassesco, MS; Pezuk, JA; Roberto, GM; Salomão, KB; Scrideli, CA; Tone, LG, 2018
)
0.48
" Drug interactions showed dissimilar results with antagonistic effects with any drug combination in MCF-7 and clear synergic interactions between both PLK1 inhibitors and cisplatin, temozolomide or doxorubicin in Hs578T, which is TP53 mutated."( PLK1 Inhibition Radiosensitizes Breast Cancer Cells, but Shows Low Efficacy as Monotherapy or in Combination with other Cytotoxic Drugs.
Brassesco, MS; Pezuk, JA; Roberto, GM; Salomão, KB; Scrideli, CA; Tone, LG, 2018
)
0.48
" Nonetheless, despite overexpressing PLK1, in our model, expressive results after its inhibition were only seen through clonogenic assays or when BI 6727 and GSK461364 were combined with ionizing radiation."( PLK1 Inhibition Radiosensitizes Breast Cancer Cells, but Shows Low Efficacy as Monotherapy or in Combination with other Cytotoxic Drugs.
Brassesco, MS; Pezuk, JA; Roberto, GM; Salomão, KB; Scrideli, CA; Tone, LG, 2018
)
0.48
" Through in vitro growth inhibition studies, Western blot analysis for the expression and activation of key regulators of cell growth and survival and gene silencing studies, we specifically examined the ability of these agents to induce cytotoxicity through the activation of apoptosis and their capacity to interact and modulate the expression and phosphorylation of Aurora kinases."( Targeted Polo-like Kinase Inhibition Combined With Aurora Kinase Inhibition in Pediatric Acute Leukemia Cells.
Boklan, J; Dunn, SE; Hofmann, B; Jayanthan, A; Meier-Stephenson, V; Narendran, A; Perinpanayagam, M; Trippett, TM; Truong, TH, 2019
)
0.51
" This phase 1 trial investigated the maximum tolerated dose (MTD), safety, pharmacokinetics, and anti-leukemic activity of volasertib in combination with decitabine in AML patients aged ≥ 65 years."( Phase 1 dose escalation trial of volasertib in combination with decitabine in patients with acute myeloid leukemia.
Borthakur, G; Cortes, J; Fagan, N; Kantarjian, H; Podoltsev, N; Rajeswari, S; Stahl, M; Taube, T; Uy, GL; Zeidan, AM, 2021
)
0.62
"This drug-drug interaction study determined whether the metabolism and distribution of the Polo-like kinase 1 inhibitor, volasertib, is affected by co-administration of the P-glycoprotein and cytochrome P-450 3A4 inhibitor, itraconazole."( Potential Drug-Drug Interactions with Combination Volasertib + Itraconazole: A Phase I, Fixed-sequence Study in Patients with Solid Tumors.
Chizhikov, E; Fritsch, H; Lang, I; Liptai, B; Liu, D; Taube, T, 2020
)
0.56

Bioavailability

ExcerptReferenceRelevance
" Because of their unique chemical versatility and unusually high bioavailability these two transition metals have been incorporated into the active sites of enzymes over the course of evolution."( Molybdenum and tungsten in biology.
Hille, R, 2002
)
0.31
" Collectively, these findings suggest that in diabetic arterioles, due to the reduced bioavailability of BH(4), the synthesis of NO by eNOS is limited, resulting in a reduced flow-induced dilation, a mechanism that may also be responsible for the development of diabetic microangiopathy and exacerbation of other vascular diseases."( Lack of nitric oxide mediation of flow-dependent arteriolar dilation in type I diabetes is restored by sepiapterin.
Bagi, Z; Koller, A,
)
0.13
"GS-9620 [8-(3-(pyrrolidin-1-ylmethyl)benzyl)-4-amino-2-butoxy-7,8-dihydropteridin-6(5H)-one] is a potent, orally bioavailable small-molecule agonist of Toll-like receptor 7 (TLR7) developed for finite treatment of chronic hepatitis B viral (HBV) infection, with the goal of inducing a liver-targeted antiviral effect without inducing the adverse effects associated with current systemic interferon-α (IFN-α) therapies."( Pharmacokinetic and pharmacodynamic properties of GS-9620, a novel Toll-like receptor 7 agonist, demonstrate interferon-stimulated gene induction without detectable serum interferon at low oral doses.
Fosdick, A; Frey, CR; Halcomb, RL; Hesselgesser, J; Pflanz, S; Tumas, DB; Wolfgang, G; Zheng, J, 2014
)
0.4
" This study determined the maximum tolerated dose (MTD) and pharmacokinetics of volasertib combined with nintedanib, a potent and orally bioavailable triple angiokinase inhibitor, in patients with advanced solid tumors."( A phase I, dose-escalation study of volasertib combined with nintedanib in advanced solid tumors.
Cascinu, S; Clementi, L; de Braud, F; De Pas, T; Liu, D; Pilz, K; Sikken, P; Spitaleri, G, 2015
)
0.42
" We here assessed the therapeutic efficacy of the orally bioavailable BRD4 inhibitor, MK-8628, in preclinical models of medulloblastoma."( Synergistic activity of BET inhibitor MK-8628 and PLK inhibitor Volasertib in preclinical models of medulloblastoma.
Althoff, K; Bei, Y; Deubzer, HE; Eggert, A; Garcia, HD; Han, Y; Henssen, AG; Künkele, A; Lindner, S; Lissat, A; Odersky, A; Schramm, A; Schulte, JH; Timme, N, 2019
)
0.51
" If this is the case, then prolonged bioavailability in the tumor should significantly increase the efficacy of antimitotic agents."( Calibrated liposomal release of the anti-mitotic agent BI-2536 increases the targeting of mitotic tumor cells.
Ann Matthews, A; Cheong, I; Goh, SMP; Ng, CZ; Sum, R; Xu, A; Yap, LW, 2020
)
0.56

Dosage Studied

ExcerptRelevanceReference
"Eleven lots of parenteral methotrexate (MTX) dosage forms from two manufactures have been analyzed and found to be 93."( Separation and identification of impurities in parenteral methotrexate dosage forms.
Azarnoff, DL; Hignite, CE; Shen, DD, 1978
)
0.26
" Although there may be other molecular differences between the heterochromatic regions of the recombinants, the most obvious is the dosage of NO."( Nucleolus organizer-suppressed position-effect variegation in Drosophila melanogaster.
DeSalle, R; Spofford, JB, 1991
)
0.28
" In order to evaluate potentially small complementation or dosage effects, mutant stains were made coisogenic for 3R."( Molybdenum hydroxylases in Drosophila. III. Further characterization of the low xanthine dehydrogenase gene.
Baldwin, MC; Finnerty, V; Schott, DR, 1986
)
0.27
" Epidermal suction blister tissues were taken before (0 h) and after (24 and 72 h) UVB exposure with a standardized dosage [1 minimal erythema dose (MED)]."( Pteridines in the control of pigmentation.
Beazley, W; Bünz, A; Körner, C; Schallreuter, KU; Schulz-Douglas, V, 1997
)
1.74
" Dose-response curves were investigated in response to the endothelium-dependent agonists histamine, serotonin, and acetylcholine (for pigs, substance P) and to the endothelium-independent agonist sodium nitroprusside (SNP) under control conditions and before and after incubation of the vessels with sepiapterin (substrate for BH4 synthesis)."( Endothelial dysfunction of coronary resistance arteries is improved by tetrahydrobiopterin in atherosclerosis.
Amann, K; Bleeke, T; Kübler, W; Tiefenbacher, CP; Vahl, C; Vogt, A, 2000
)
0.31
" The inhibitory effect of the high dosages of OE(2) correlated with an increase in the apparent K(m) values (decreased affinity) for both substrate and cofactor, and a decrease in the V(max) compared with the lower dosage groups."( Effects of ovariectomy and oestradiol-17beta replacement on brain tyrosine hydroxylase in the catfish Heteropneustes fossilis: changes in in vivo activity and kinetic parameters.
Chaube, R; Joy, KP, 2002
)
0.31
" The extent of rescue was dependent on the dosage of transgenic CG6781."( Identification and characteristics of the structural gene for the Drosophila eye colour mutant sepia, encoding PDA synthase, a member of the omega class glutathione S-transferases.
Ahn, C; Kim, J; Kim, K; Kim, S; Suh, H; Yim, J, 2006
)
0.33
" As a functional benefit, interventional dosing schedules of this inhibitor also reduced airway hyper-responsiveness."( Aerosolized phosphoinositide 3-kinase gamma/delta inhibitor TG100-115 [3-[2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol] as a therapeutic candidate for asthma and chronic obstructive pulmonary disease.
Acevedo, LM; Cheresh, DA; Dellamary, L; Dneprovskaia, E; Doukas, J; Eide, L; Martin, M; Noronha, G; Racanelli-Layton, A; Soll, R; Stebbins, K; Wrasidlo, W, 2009
)
0.35
" as well as oral formulations, adding flexibility to dosing schedules."( BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity.
Adolf, GR; Baum, A; Garin-Chesa, P; Grauert, M; Haslinger, C; Hoffmann, M; Quant, J; Rudolph, D; Steegmaier, M, 2009
)
0.35
"To investigate the efficacy, safety, and pharmacokinetics of two dosing schedules of BI 2536, a novel polo-like kinase-1 inhibitor, in patients with relapsed stage IIIB/IV non-small cell lung cancer."( The efficacy and safety of BI 2536, a novel Plk-1 inhibitor, in patients with stage IIIB/IV non-small cell lung cancer who had relapsed after, or failed, chemotherapy: results from an open-label, randomized phase II clinical trial.
Frickhofen, N; Fritsch, H; Gaschler-Markefski, B; Hanft, G; Kortsik, C; Munzert, G; Reck, M; Schuler, M; Sebastian, M; von Pawel, J; Waller, CF, 2010
)
0.36
" There was a trend in favor of the days 1 to 3 dosing schedule in quality of life."( The efficacy and safety of BI 2536, a novel Plk-1 inhibitor, in patients with stage IIIB/IV non-small cell lung cancer who had relapsed after, or failed, chemotherapy: results from an open-label, randomized phase II clinical trial.
Frickhofen, N; Fritsch, H; Gaschler-Markefski, B; Hanft, G; Kortsik, C; Munzert, G; Reck, M; Schuler, M; Sebastian, M; von Pawel, J; Waller, CF, 2010
)
0.36
" The MTD for the second dosing schedule was not determined; a 225-mg dose was well tolerated."( An open-label, phase I study of the polo-like kinase-1 inhibitor, BI 2536, in patients with advanced solid tumors.
Al-Batran, SE; Fritsch, H; Hochhaus, A; Hofheinz, RD; Jäger, E; Munzert, G; Reichardt, VL; Trommeshauser, D, 2010
)
0.36
" When dosed orally in rats, compound 37 demonstrated a 41-45% reduction of pS129-α-synuclein levels in the cerebral cortex."( Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors.
Anderson, JP; Artis, DR; Aubele, DL; Baker, J; Bergeron, M; Beroza, P; Bova, MP; Bowers, S; Chan, W; Dappen, MS; Diep, L; Fauss, D; Fitzgerald, K; Galemmo, RA; Hoffman, J; Hom, RK; Konradi, AW; Motter, R; Neitz, RJ; Pandya, D; Ren, Z; Ruslim, L; Sealy, JM; Sham, HL; Tam, D; Tanaka, P; Tonn, G; Truong, AP; Ye, M; Zhang, H; Zhu, YL, 2013
)
0.39
" Our data discriminated between alternative mechanisms that compromise drug sensitivity to paclitaxel and revealed an unexpected bell-shaped dose-response curve for BI2536, a highly selective inhibitor of Polo-like kinases."( Differential determinants of cancer cell insensitivity to antimitotic drugs discriminated by a one-step cell imaging assay.
Benes, C; Florian, S; Mitchison, TJ; Moerke, N; Shamu, C; Tang, Y; Xie, T, 2013
)
0.39
"These data support further development of volasertib and a harmonised dosing for Asian and Caucasian patients."( A phase I study of two dosing schedules of volasertib (BI 6727), an intravenous polo-like kinase inhibitor, in patients with advanced solid malignancies.
Cheng, AL; Fritsch, H; Hsu, CH; Huang, DC; Lin, CC; Lu, YS; Su, WC; Su, WP; Taube, T; Voss, F; Yang, JC; Yeh, KH; Yen, CJ, 2014
)
0.4
"After evaluating the pharmacokinetics, pharmacodynamics and tolerability of oral GS-9620 in uninfected woodchucks, adult woodchucks chronically infected with WHV (n = 7 per group) were dosed with GS-9620 or placebo for 4 or 8 weeks with different treatment schedules."( Sustained efficacy and seroconversion with the Toll-like receptor 7 agonist GS-9620 in the Woodchuck model of chronic hepatitis B.
AlDeghaither, D; Baldwin, BH; Bellezza, CA; Cote, PJ; Daffis, S; Fletcher, SP; Fosdick, A; Halcomb, R; Li, L; Liu, KH; Menne, S; Tennant, BC; Thampi, L; Tumas, DB; Wolfgang, GH; Yue, P; Zheng, J, 2015
)
0.42
" Overall, a transient dose-dependent induction of peripheral ISG15 gene expression was observed peaking within 48 hours of dosing followed by return to baseline levels within seven days."( The oral toll-like receptor-7 agonist GS-9620 in patients with chronic hepatitis B virus infection.
Cheng, W; Coffin, CS; Fedorak, RN; Freilich, B; Gaggar, A; Gane, EJ; Garrison, KL; Gordon, SC; Kim, YJ; Kottilil, S; Lim, YS; Mani Subramanian, G; Massetto, B; McHutchison, JG; Pflanz, S; Roberts, S; Sicard, E; Visvanathan, K; Ye, Z, 2015
)
0.42
"The MCF10A progressive breast cancer model, including sequentially derived MCF10A (benign), MCF10AT (premalignant), and MCF10CA1a (malignant) cell lines were dosed with 0, 100, and 250 mg/L folic acid."( Establishing pteridine metabolism in a progressive isogenic breast cancer cell model.
Burton, C; Foulks, Z; Rasmussen, L; Shi, H, 2021
)
0.62
" Folic acid dosing increased extracellular levels of pterin, 6-hydroxylumazine, xanthopterin, 6-hydroxymethylpterin, and 6-carboxypterin in a dose-dependent manner."( Establishing pteridine metabolism in a progressive isogenic breast cancer cell model.
Burton, C; Foulks, Z; Rasmussen, L; Shi, H, 2021
)
0.62
"This study sought to elucidate the pteridine biosynthetic pathway in a progressive breast cancer model via direct pteridine dosing to determine how pteridine metabolism changes with tumorigenicity."( Establishing pteridine metabolism in a progressive isogenic breast cancer cell model - part II.
Burton, C; Foulks, Z; Rasmussen, L; Shi, H; Wu, J, 2022
)
0.72
"First, MCF10AT breast cancer cells were dosed individually with 15 pteridines to determine which pteridines were being metabolized and what metabolic products were being produced."( Establishing pteridine metabolism in a progressive isogenic breast cancer cell model - part II.
Burton, C; Foulks, Z; Rasmussen, L; Shi, H; Wu, J, 2022
)
0.96
"05) with respect to tumorigenicity following dosing with pterin and sepiapterin, respectively."( Establishing pteridine metabolism in a progressive isogenic breast cancer cell model - part II.
Burton, C; Foulks, Z; Rasmussen, L; Shi, H; Wu, J, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (4)

ClassDescription
pteridines
mancude organic heterobicyclic parent
azaarene
ortho-fused heteroareneAn ortho-fused compound in which at least one of the rings contains at least one heteroatom.
[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]

Research

Studies (2,743)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901198 (43.67)18.7374
1990's405 (14.76)18.2507
2000's469 (17.10)29.6817
2010's572 (20.85)24.3611
2020's99 (3.61)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 46.11

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 Index46.11 (24.57)
Research Supply Index7.95 (2.92)
Research Growth Index4.50 (4.65)
Search Engine Demand Index76.22 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (46.11)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials46 (1.65%)5.53%
Reviews197 (7.06%)6.00%
Case Studies107 (3.83%)4.05%
Observational2 (0.07%)0.25%
Other2,440 (87.39%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]