Page last updated: 2024-12-08

alpha-cyclodextrin

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

Description

alpha-cyclodextrin : A cycloamylose composed of six alpha-(1->4) linked D-glucopyranose units. [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]

Cross-References

ID SourceID
PubMed CID444913
CHEMBL ID1230813
CHEBI ID40585
SCHEMBL ID24981
MeSH IDM0101690

Synonyms (88)

Synonym
e-457
alpha cyclodextrin
ins-457
CHEMBL1230813
ringdex-a
cavamax w6
oristar acd
dexy pearl .alpha.-100
ins no.457
cavamax w 6 food
celdex a 100
hexakis(hydroxymethyl)[?]dodecol
10016-20-3
cyclomaltohexose
.alpha.-cyclodextrin
nsc-269470
alfadex
alpha-cyclodextrin
NCGC00090767-01
cyclohexapentylose
alfadex [inn]
alpha-dextrin
nsc 269470
dextrin, alpha-cyclo
alpha-schardinger dextrin
alpha-cycloamylose
alfadexum [inn-latin]
einecs 233-007-4
alpha-cyclodextrin, powder, bioreagent, suitable for cell culture, >=98%
alpha-cyclodextrin, >=98%
CHEBI:40585 ,
DB01909
ACX ,
alpha-cyclodextrin (cyclohexa-amylose)
NCGC00090767-02
MLS001074882
smr000568406
C-9100
3CK7
D08846
alfadex (inn/nf)
NCGC00090767-03
NCGC00090767-04
ec 233-007-4
alfadexum
z1lh97ktrm ,
alfadex [inn:ban:nf]
unii-z1lh97ktrm
NCGC00253988-01
NCGC00258804-01
tox21_201252
tox21_300302
dtxcid5010698
tox21_111015
dtxsid7030698 ,
cas-10016-20-3
HMS2232K21
alfadex [ii]
alfadex [mart.]
alfadex [ep monograph]
alpha-cyclodextrin [fcc]
.alpha.-cyclodextrin [mi]
alfadex [who-dd]
alpha cyclodextrin [usp-rs]
4FEM
AKOS015900446
SCHEMBL24981
2ZYM
3ZST
HFHDHCJBZVLPGP-RWMJIURBSA-N
alfadex, european pharmacopoeia (ep) reference standard
alpha-cyclodextrin, produced by wacker chemie ag, burghausen, germany, >=99.0% (hplc)
alpha-cyclodextrin, produced by wacker chemie ag, burghausen, germany, life science, 98.0-101.0% cyclodextrin basis (hplc)
alpha cyclodextrin, united states pharmacopeia (usp) reference standard
alpha-cyclodextrin, purum, >=98.0% (hplc)
alpha-cyclodextrin, fg, produced by wacker chemie ag, burghausen, germany, food, >=98% (on dry substance)
anti-configured tubular 2-((2-ethoxy-13,113,513-tris(2-ethoxy-2-oxoethoxy)-8-hydroxy-116h,516h-3,7-diaza-1(4,12)-8,16-methanodinaphtho[2,1-d:1',2'-g][1,3]dioxocina-5(4,12)-dinaphtho[2,1-d:1',2'-g][1,3]dioxocinacyclooctaphane-2,7-dien-53-yl)oxy)acetic acid
HY-B1513
CS-0013302
Q27104460
AS-10392
isoquinoliniumchloride
I11498
BP-31069
A897566
alpha -cyclodextrin
?cyclohexapentylose
alfadex; cyclohexakis-(1?4)-(?-d-glucopyranosyl) (cyclomaltohexaose); cyclohexakis-(1?4)-(?-d-glucopyranosyl) ?-cyclodextrin

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" With both vehicles CTFT and alpha 2u-globulin were found to accumulate in the male rat kidney after 14 days of exposure and a dose-related toxic nephropathy was observed at dose of 50 mg/kg or higher."( Application of molecular encapsulation for toxicology studies: comparative toxicity of p-Chloro-alpha, alpha, alpha-trifluorotoluene in alpha-cyclodextrin vehicle versus corn oil vehicle in male and female Fischer 344 rats and B6C3F1 mice.
Carlton, T; Corniffe, G; Elwell, MR; Goehl, TJ; Jameson, CW; Leininger, JR; Thompson, MB; Yuan, J, 1992
)
0.28
" In this study, the PDsuc-appended alpha-CyD ester conjugate (PDsuc/alpha-CyD conjugate) was intracolonically administered to rats with 2,4,6-trinitrobenzensulfonic acid-induced colitis, and its antiinflammatory and systemic adverse effects were compared with those of prednisolone (PD) alone and the PD/2-hydroxypropyl-beta-CyD complex (PD/HP-beta-CyD complex), which is a noncovalent inclusion complex."( Prednisolone-appended alpha-cyclodextrin: alleviation of systemic adverse effect of prednisolone after intracolonic administration in 2,4,6-trinitrobenzenesulfonic acid-induced colitis rats.
Arima, H; Hirayama, F; Uekama, K; Yano, H, 2001
)
0.31
" In this study, the anti-inflammatory effect and systemic side effect of the PD succinate/alpha-cyclodextrin (PDsuc/alpha-CyD) ester conjugate after oral administration were studied using IBD model rats."( Colon-specific delivery of prednisolone-appended alpha-cyclodextrin conjugate: alleviation of systemic side effect after oral administration.
Arima, H; Hirayama, F; Kamada, M; Uekama, K; Yano, H, 2002
)
0.31
" In conclusion, no adverse effects were observed at alpha-CD intakes of up to 20% of the diet, the highest dose level tested at which the rats consumed about 13 g/kg bw/day."( Embryotoxicity and teratogenicity study with alpha-cyclodextrin in rats.
Bär, A; Waalkens-Berendsen, DH, 2004
)
0.32
" It was concluded that dietary alpha-CD is generally well tolerated by pregnant rabbits, has no adverse effect on maternal reproductive performance and is not embryotoxic, fetotoxic, or teratogenic at dietary concentrations of up to 20%, the highest dose level tested."( Embryotoxicity and teratogenicity study with alpha-cyclodextrin in rabbits.
Bär, A; Smits-Van Prooije, AE; Waalkens-Berendsen, DH, 2004
)
0.32
" However, the concentration of α-cyclodextrin used may be very high in these cases, and its toxic attributes have to be seriously considered."( Evaluation of the Cytotoxicity of α-Cyclodextrin Derivatives on the Caco-2 Cell Line and Human Erythrocytes.
Bácskay, IK; Bocsik, A; Deli, M; Fehér, P; Félix, C; Fenyvesi, É; Fenyvesi, F; Gesztelyi, R; Perret, F; Róka, E; Szente, L; Ujhelyi, Z; Váradi, J; Vecsernyés, M, 2015
)
0.42

Pharmacokinetics

ExcerptReferenceRelevance
" The area under the serum G-CSF concentration-time curve (AUC, a pharmacokinetic parameter) and the area under the increased total blood leukocyte count-time curve (AUL, a pharmacodynamic parameter) increased with increase of dose of rhG-CSF administered intranasally."( Pharmacokinetics and pharmacodynamics of recombinant human granulocyte colony-stimulating factor (rhG-CSF) following intranasal administration in rabbits.
Kikuchi, R; Kiriyama, M; Maruyama, K; Matsumoto, M; Matsumoto, Y; Nakagawa, K; Nomura, H; Watanabe, Y, 1995
)
0.29

Bioavailability

Alpha-cyclodextrin was chosen as an aqueous phase ligand, as it is frequently used in drug formulations to enhance solubility and bioavailability of drug compounds. In combination with xanthan gum, alpha-cyclodesxtrin reduced the first-pass metabolism of morphine in the rectal mucosa.

ExcerptReferenceRelevance
" Dose proportionality for CTFT was established up to 400 mg/kg and bioavailability was shown to be complete for both vehicles."( Application of molecular encapsulation for toxicology studies: toxicokinetics of p-chloro-alpha,alpha,alpha-trifluorotoluene in alpha-cyclodextrin or corn oil vehicles in male F344 rats.
Collins, BJ; Goehl, TJ; Jameson, CW; Judd, L; Purdie, W; Yuan, JM, 1991
)
0.28
" Plasma concentrations of the hormone were determined until 240 min post administration by ELISA, and the absolute bioavailability was estimated to be in the vicinity of 20%."( Epithelial transport and bioavailability of intranasally administered human growth hormone formulated with the absorption enhancers didecanoyl-L-alpha-phosphatidylcholine and alpha-cyclodextrin in rabbits.
Agerholm, C; Bastholm, L; Elling, F; Johansen, PB; Nielsen, MH, 1994
)
0.29
" In combination with xanthan gum, alpha-cyclodextrin reduced the first-pass metabolism of morphine in the rectal mucosa and by the liver and improved the apparent rectal bioavailability of the opioid about 4 fold."( Combination effects of alpha-cyclodextrin and xanthan gum on rectal absorption and metabolism of morphine from hollow-type suppositories in rabbits.
Irie, T; Kondo, T; Uekama, K, 1996
)
0.29
" The intestinal absorption rate measured by an in situ recirculating perfusion technique was higher for a complex with higher lipophilicity."( Significance of water solubility in the gastrointestinal absorption of trans-bis(n-valerato)(1R,2R-cyclohexanediamine)(oxalato)platinum(IV), an orally active antitumor platinum complex, and its analogs.
Akiyama, N; Eriguchi, M; Hayakawa, K; Kidani, Y; Kizu, R; Matsuzawa, A; Nakanishi, T; Takeda, Y; Yamamoto, S, 1998
)
0.3
" In spite of its poor solubility, PZQ is well absorbed across the gastrointestinal tract, but large doses are required to achieve adequate concentrations at the target sites."( Improvement of the in vitro dissolution of praziquantel by complexation with alpha-, beta- and gamma-cyclodextrins.
Becket, G; Schep, LJ; Tan, MY, 1999
)
0.3
" HCG was not detected in plasma when only hCG was administered rectally, even at a higher dose (4,000 IU/kg body weight) than intravenous injection, because of its low bioavailability due to high molecular weight or degradation by proteolytic activity."( Pharmacokinetics and pharmacodynamics of human chorionic gonadotropin (hCG) after rectal administration of hollow-type suppositories containing hCG.
Fujii, M; Hirosawa, I; Kowari, K; Kurai, H; Utoguchi, N; Watanabe, Y, 2002
)
0.31
"In the present work we investigated the possibility of improving dehydroepiandrosterone (DHEA) solubility and bioavailability by high-energy cogrinding with alpha-cyclodextrin (alpha-Cd) in the presence or absence of different auxiliary substances (glycine, biomaltodextrin, poly(vinyl pyrrolidone), poly(ethylene glycol) 400)."( Enhancement of dehydroepiandrosterone solubility and bioavailability by ternary complexation with alpha-cyclodextrin and glycine.
Allolio, B; Carli, F; Cirri, M; Guenther, S; Mora, PC; Mura, P, 2003
)
0.32
"To explore the use of cyclodextrins (CD) to form inclusion complexes with beta-lapachone (beta-lap) to overcome solubility and bioavailability problems previously noted with this drug."( Enhancement of solubility and bioavailability of beta-lapachone using cyclodextrin inclusion complexes.
Beman, M; Boothman, DA; Bornmann, WG; Bruening, A; Gao, J; Nasongkla, N; Ray, D; Wiedmann, AF, 2003
)
0.32
" Biologic activity and bioavailability of beta-lap inclusion complexes were investigated by in vitro cytotoxicity studies with MCF-7 cells and by in vivo lethality studies with C57Blk/6 mice (18-20 g)."( Enhancement of solubility and bioavailability of beta-lapachone using cyclodextrin inclusion complexes.
Beman, M; Boothman, DA; Bornmann, WG; Bruening, A; Gao, J; Nasongkla, N; Ray, D; Wiedmann, AF, 2003
)
0.32
" Encapsulation with alpha-cyclodextrin improves (i) the chemical stability of FA against UVB stress (10 MED [Minimal Erythemal Dose: 1 MED=25 mJ/cm(2) for skin phototype II: 30]), since no degradation products are formed after irradiation, and (ii) the bioavailability of FA on the skin, slowing its delivery (Strainer cell model)."( Non-covalent inclusion of ferulic acid with alpha-cyclodextrin improves photo-stability and delivery: NMR and modeling studies.
Andreassi, M; Anselmi, C; Beretta, G; Buonocore, A; Centini, M; Facino, RM; Gaggelli, N; Maggiore, M, 2008
)
0.35
" Alpha-cyclodextrin was chosen as an aqueous phase ligand, as it is frequently used in drug formulations to enhance solubility and bioavailability of drug compounds."( Effect of alpha-cyclodextrin on drug distribution studied by electrochemistry at interfaces between immiscible electrolyte solutions.
Deryabina, MA; Hansen, SH; Jensen, H; Østergaard, J, 2009
)
0.35
" Lipid-based formulations showed an increase of relative bioavailability of IND versus Indocid®."( Formulations based on alpha cyclodextrin and soybean oil: an approach to modulate the oral release of lipophilic drugs.
Bochot, A; Bourasset, F; Domergue-Dupont, V; Fattal, E; Gueutin, C; Hamoudi, MC; Nicolas, V, 2012
)
0.38
" Therefore, beads with high drug loading and improved oral bioavailability have great potential for oral delivery of poorly water-soluble drugs and lipophilic drugs."( [Research progress of self-assembled beads drug delivery system prepared from cyclodextrins and oils].
Liu, C; Yi, T, 2012
)
0.38
" In rats, the oral bioavailability of isotretinoin is twofold enhanced with uncoated beads as compared to the lipid content of a soft capsule."( Oil-cyclodextrin based beads for oral delivery of poorly-soluble drugs.
Bochot, A; Hamoudi, MC, 2014
)
0.4
"Levodopa (LEVO) as the gold standard in the treatment of Parkinson's disease is usually administrated per os but its bioavailability is low."( Interaction Studies Between Levodopa and Different Excipients to Develop Coground Binary Mixtures for Intranasal Application.
Alapi, T; Ambrus, R; Bartos, C; Katona, G; Kiss, T; Szabó-Révész, P; Varga, G, 2019
)
0.51
"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

Dosage Studied

ExcerptRelevanceReference
" The hepatocellular hypertrophy and cytoplasmic vacuolation of the adrenal cortex which appeared in dosed male and female rats were also found to be independent of vehicle."( Application of molecular encapsulation for toxicology studies: comparative toxicity of p-Chloro-alpha, alpha, alpha-trifluorotoluene in alpha-cyclodextrin vehicle versus corn oil vehicle in male and female Fischer 344 rats and B6C3F1 mice.
Carlton, T; Corniffe, G; Elwell, MR; Goehl, TJ; Jameson, CW; Leininger, JR; Thompson, MB; Yuan, J, 1992
)
0.28
" Serial blood samples were taken from a cannulated jugular vein for up to 52 hr after dosing and the CTFT concentrations in whole blood were determined by gas chromatography."( Application of molecular encapsulation for toxicology studies: toxicokinetics of p-chloro-alpha,alpha,alpha-trifluorotoluene in alpha-cyclodextrin or corn oil vehicles in male F344 rats.
Collins, BJ; Goehl, TJ; Jameson, CW; Judd, L; Purdie, W; Yuan, JM, 1991
)
0.28
" In order to achieve a better understanding of the dosage regimen and the effectiveness of intranasally administered rhG-CSF in inducing leukopoiesis, we investigated rhG-CSF absorption and blood leukocyte dynamics with respect to dose in rabbits."( Pharmacokinetics and pharmacodynamics of recombinant human granulocyte colony-stimulating factor (rhG-CSF) following intranasal administration in rabbits.
Kikuchi, R; Kiriyama, M; Maruyama, K; Matsumoto, M; Matsumoto, Y; Nakagawa, K; Nomura, H; Watanabe, Y, 1995
)
0.29
" A long-term oral dosage form would be favorable, but this type of medication has not been developed yet because of the important first-pass effect and low and variable bioavailability."( Skin permeation study of dehydroepiandrosterone (DHEA) compared with its alpha-cyclodextrin complex form.
Ceschel, GC; Lombardi Borgia, S; Maffei, P; Mora, PC; Ronchi, C, 2002
)
0.31
" The observed complexation may substantially modify properties of bupivacaine hydrochloride dosage forms with sufficient concentration of cyclodextrin but bupivacaine cations are readily released from the weak cyclodextrin complexes by dilution."( Bupivacaine hydrochloride complexation with some alpha- and beta-cyclodextrins studied by potentiometry with membrane electrodes.
Bieliková, Z; Demko, M; Kaclík, P; Kopecký, F; Vojteková, M, 2004
)
0.32
"This study evaluated the dose-response effects of alpha-cyclodextrin, a cyclic oligosaccharide, on the glycaemic and insulinaemic responses to the consumption of a standard carbohydrate meal."( Dose-dependent inhibition of the post-prandial glycaemic response to a standard carbohydrate meal following incorporation of alpha-cyclodextrin.
Buckley, JD; Howe, PR; Murphy, KJ; Thorp, AA, 2006
)
0.33
"A rapid and nondestructive analytical technique is critical for the analysis of cyclodextrin inclusion complexes in solid dosage forms."( Solid-State Analysis of Alpha-Cyclodextrin Inclusion Complexes Using Low-Frequency Raman Spectroscopy.
Carriere, J; Fukami, T; Hisada, H; Inoue, M; Koide, T; Roy, A; Takatori, K, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
cyclodextrinA macrocycle composed of five or more D-glucopyranose units bonded via (1->4)-linkages.
[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]

Protein Targets (24)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency10.00000.004023.8416100.0000AID485290
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency79.43280.631035.7641100.0000AID504339
GLI family zinc finger 3Homo sapiens (human)Potency28.24210.000714.592883.7951AID1259368; AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency5.48330.000221.22318,912.5098AID743036
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
thyroid stimulating hormone receptorHomo sapiens (human)Potency10.00000.001318.074339.8107AID926; AID938
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency32.40440.001022.650876.6163AID1224838
progesterone receptorHomo sapiens (human)Potency22.94050.000417.946075.1148AID1346795
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency41.33790.003041.611522,387.1992AID1159552; AID1159553; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency25.96810.000817.505159.3239AID1159527
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency22.10890.001530.607315,848.9004AID1224841; AID1224848; AID1224849
estrogen nuclear receptor alphaHomo sapiens (human)Potency24.24320.000229.305416,493.5996AID588514; AID743069; AID743075; AID743079
thyroid stimulating hormone receptorHomo sapiens (human)Potency22.94050.001628.015177.1139AID1224843
Histone H2A.xCricetulus griseus (Chinese hamster)Potency53.41200.039147.5451146.8240AID1224845
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency28.33680.000627.21521,122.0200AID743202; AID743219
gemininHomo sapiens (human)Potency6.99360.004611.374133.4983AID624296; AID624297
lamin isoform A-delta10Homo sapiens (human)Potency1.25890.891312.067628.1838AID1487
Cellular tumor antigen p53Homo sapiens (human)Potency40.79470.002319.595674.0614AID651631
[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 B, Putative Glucanohydrolase Pep1a Glge Isoform 1Streptomyces coelicolorIC50 (µMol)19,000.000019,000.000019,000.000019,000.0000AID977608
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Solute-binding proteinThermoactinomyces vulgarisKd0.73000.73000.96501.2000AID977611
Chain A, Solute-binding proteinThermoactinomyces vulgarisKd0.73000.73000.96501.2000AID977611
Chain B, SusDBacteroides thetaiotaomicron VPI-5482Kd89.000089.0000117.5000146.0000AID977611
Chain A, SusDBacteroides thetaiotaomicron VPI-5482Kd89.000089.0000117.5000146.0000AID977611
Chain A, SusDBacteroides thetaiotaomicron VPI-5482Kd89.000089.0000117.5000146.0000AID977611
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (124)

Processvia Protein(s)Taxonomy
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (34)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (19)

Processvia Protein(s)Taxonomy
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (15)

Assay IDTitleYearJournalArticle
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2009The FEBS journal, Jun, Volume: 276, Issue:11
Crystal structures of open and closed forms of cyclo/maltodextrin-binding protein.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID651635Viability Counterscreen for Primary 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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
AID293631Artificial HSP60-like chaperone activity assessed as prevention of citrate synthase thermal aggregation2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
HSP90-like artificial chaperone activity based on indole beta-cyclodextrin.
AID1351281Solubility of the compound in water assessed per 100 ml2018European journal of medicinal chemistry, Jan-20, Volume: 144Polymeric bile acid sequestrants: Review of design, in vitro binding activities, and hypocholesterolemic effects.
AID1337347Aqueous solubility of the compound at room temperature measured per 100 ml of solution2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of novel pentacyclic triterpene α-cyclodextrin conjugates as HCV entry inhibitors.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2011The Journal of biological chemistry, Nov-04, Volume: 286, Issue:44
Structure of Streptomyces maltosyltransferase GlgE, a homologue of a genetically validated anti-tuberculosis target.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2008Structure (London, England : 1993), Jul, Volume: 16, Issue:7
Starch catabolism by a prominent human gut symbiont is directed by the recognition of amylose helices.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2012The Journal of biological chemistry, Oct-05, Volume: 287, Issue:41
Multidomain Carbohydrate-binding Proteins Involved in Bacteroides thetaiotaomicron Starch Metabolism.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (597)

TimeframeStudies, This Drug (%)All Drugs %
pre-199031 (5.19)18.7374
1990's79 (13.23)18.2507
2000's226 (37.86)29.6817
2010's233 (39.03)24.3611
2020's28 (4.69)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials9 (1.48%)5.53%
Reviews8 (1.31%)6.00%
Case Studies0 (0.00%)4.05%
Observational1 (0.16%)0.25%
Other591 (97.04%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]