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dehydroepiandrosterone sulfate

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Description

Dehydroepiandrosterone Sulfate: The circulating form of a major C19 steroid produced primarily by the ADRENAL CORTEX. DHEA sulfate serves as a precursor for TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

dehydroepiandrosterone sulfate : A steroid sulfate that is the 3-sulfooxy derivative of dehydroepiandrosterone. [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 CID12594
CHEMBL ID259898
CHEBI ID16814
SCHEMBL ID27640
MeSH IDM0028759

Synonyms (103)

Synonym
mylis
57b09q7fjr ,
unii-57b09q7fjr
androst-5-en-17-one, 3-beta-hydroxy-, hydrogen sulfate
androst-5-en-17-one, 3-(sulfooxy)-, (3-beta)-
dehydroisoandrosterone-3-sulfate
3beta-hydroxyandrost-5-en-17-one-3-sulfate
(3-beta)-3-(sulfooxy)androst-5-en-17-one
5-androsten-3beta-sulfate-17-one
17-oxoandrost-5-en-3beta-yl hydrogen sulfate
CHEBI:16814 ,
(3beta)-17-oxoandrost-5-en-3-yl hydrogen sulfate
LOPAC0_000379
dehydroepiandrosterone sulphate
dehydroisoandrosterone sulfate
dehydroandrosterone sulfate
androst-5-en-17-on-3beta-yl sulfate
3beta-hydroxy-5-androsten-17-one monosulfate
androst-5-ene-17-one-3beta-yl-sulfate
dehydroepiandrosterone 3beta-sulfate
androst-5-en-17-on-3beta-yl sulfuric acid
17-ketoandrost-5-en-3beta-yl sulfate
dehydroepiandrosterone monosulfate
ccris 6746
androst-5-en-17-one, 3beta-hydroxy-, hydrogen sulfate (6ci,8ci)
cmc_13438
3beta-sulfooxy-5-androsten-17-one
dehydroepiandrosterone 3-sulfate
androst-5-en-17-one, 3-(sulfooxy)-, (3beta)-
5-androsten-3-beta-sulfate-17-one
3-o-sulfodehydroepiandrosterone
3beta-hydroxy-5-androsten-17-one 3-sulfate
androst-5-en-17-one-3beta-yl sulfate
3beta-hydroxy-5-androsten-17-one sulfate
androst-5-en-17-one, 3-(sulfooxy)-, (3beta)- (9ci)
LMST05020010
dehydroepiandrosterone sulfate
C04555
651-48-9
3beta-hydroxyandrost-5-en-17-one 3-sulfate
dhea sulfate
teloin (*sodium salt*)
dehydroepiandrosterone 3-sulphate
mylis (*sodium salt*)
1099-87-2
androst-5-en-17-one, 3-(sulfooxy)-, (3.beta.)-
dhea-s
nsc72822
prasterone sulfate
[(3s,8r,9s,10r,13s,14s)-10,13-dimethyl-17-oxo-1,2,3,4,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-yl] hydrogen sulfate
dehydroepiandrosterone-sulfate
inflarest
dheas
pb-005
prasterone sulfuric acid
CHEMBL259898 ,
formylisoglutamic acid
bdbm50375559
EPITOPE ID:150912
prasterone sulphate
dhea sulphate
17-oxoandrost-5-en-3beta-yl hydrogen sulphate
DB05804
SCHEMBL27640
dehydroepiandrosterone sulfate [mi]
androst-5-en-17-one, 3.beta.-hydroxy-, hydrogen sulfate
prasterone sulfate [mart.]
genaflow
prasterone sulfate [who-dd]
10,13-dimethyl-17-oxo-3-sulfooxy-1,2,3,4,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthrene
prasterone-3-sulfate
androst-5-en-17-one, 3-(sulfooxy)-, (3b)-
DTXSID8040228
AKOS027320789
3-beta-hydroxyandrost-5-en-17-one 3-sulphate
3b-hydroxyandrost-5-en-17-one 3-sulfate
dehydroepiandrosterone-3-sulfate
3-b-hydroxyandrost-5-en-17-one 3-sulfate
(3beta)-3-(sulfooxy)-androst-5-en-17-one
3b-hydroxyandrost-5-en-17-one 3-sulphate
dehydroepiandrosterone-3-sulphate
prasterone-3-sulphate
17-oxoandrost-5-en-3-yl hydrogen sulphate
3beta-hydroxy-androst-5-en-17-one hydrogen sulfate
17-oxoandrost-5-en-3b-yl hydrogen sulfate
3beta-hydroxyandrost-5-en-17-one 3-sulphate
17-oxoandrost-5-en-3b-yl hydrogen sulphate
3b-hydroxy-androst-5-en-17-one hydrogen sulphate
3-b-hydroxyandrost-5-en-17-one 3-sulphate
3b-hydroxy-androst-5-en-17-one hydrogen sulfate
3beta-hydroxy-androst-5-en-17-one hydrogen sulphate
17-oxoandrost-5-en-3-yl hydrogen sulfate
dehydroisoandrosterone sulphate
kb60
651-48-9 (free acid)
(3s,8r,9s,10r,13s,14s)-10,13-dimethyl-17-oxo-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-3-yl hydrogen sulfate
Q2505402
CZWCKYRVOZZJNM-USOAJAOKSA-N
MS-25917
HY-113416
CS-0059419
dehydroepiandrosterone sulfate; dhea sulfate; dhea-s
17-oxo-8alpha,10alpha,13alpha,14beta-androst-5-en-3alpha-yl hydrogen sulfate

Research Excerpts

Overview

Dehydroepiandrosterone sulfate (DHEAS) is a circulating steroid produced in the adrenal cortex, brain, and gonads. It is a corticotropin-dependent adrenal androgen, which has immunostimulating and antiglucocorticoid effects.

ExcerptReferenceRelevance
"Dehydroepiandrosterone sulfate (DHEAS) is a corticotropin-dependent adrenal androgen, which has immunostimulating and antiglucocorticoid effects."( Dehydroepiandrosterone sulfate and dehydroepiandrosterone sulfate/cortisol ratio in cirrhotic patients with septic shock: another sign of hepatoadrenal syndrome?
Chen, YC; Fang, JT; Hsieh, SY; Huang, HC; Lee, FY; Lien, JM; Peng, YS; Tian, YC; Tsai, MH; Wu, CS; Yang, CW, 2017
)
2.62
"Dehydroepiandrosterone sulfate (DHEAS) is a circulating steroid produced in the adrenal cortex, brain, and gonads. "( Dehydroepiandrosterone sulfate mediates activation of transcription factors CREB and ATF-1 via a Gα11-coupled receptor in the spermatogenic cell line GC-2.
Kirch, U; Scheiner-Bobis, G; Shihan, M, 2013
)
3.28
"Dehydroepiandrosterone sulfate (DHEAS) is a precursor of testosterone and a substrate for SLCO2B1, an organic anionic transporter."( Statin Use at the Time of Initiation of Androgen Deprivation Therapy and Time to Progression in Patients With Hormone-Sensitive Prostate Cancer.
Harshman, LC; Kantoff, AM; Kantoff, PW; Lee, GS; Mucci, LA; Nakabayashi, M; Pomerantz, M; Sweeney, CJ; Valenca, L; Wang, X; Werner, L; Xie, W; Yu, Y, 2015
)
1.14
"Dehydroepiandrosterone sulfate (DHEAS) is a circulating sulfated steroid considered to be a pro-androgen in mammalian physiology. "( Dehydroepiandrosterone Sulfate Stimulates Expression of Blood-Testis-Barrier Proteins Claudin-3 and -5 and Tight Junction Formation via a Gnα11-Coupled Receptor in Sertoli Cells.
Dietze, R; Kirch, U; Papadopoulos, D; Scheiner-Bobis, G; Shihan, M, 2016
)
3.32
"Dehydroepiandrosterone sulfate (DHEA(S)) is a multi-functional steroid implicated in a broad range of biological effects, including obesity, diabetes, bone metabolism, neuroprotection, and anti-tumorigenesis. "( DHEA(S)--a novel marker in Cushing's disease.
Aberle, J; Burkhardt, T; Flitsch, J; Mengel, M; Schmidt, NO; Vettorazzi, E, 2013
)
1.83
"Dehydroepiandrosterone sulfate (DHEAS) is a 19-carbon steroid, situated along the steroid metabolic pathway. "( DHEAS as a new diagnostic tool.
Leowattana, W, 2004
)
1.77
"Dehydroepiandrosterone sulfate (DHEA-S) is a corticotropin-dependent adrenal androgen precursor that is suppressible in patients treated with ICs."( Assessment of adrenal suppression in children with asthma treated with inhaled corticosteroids: use of dehydroepiandrosterone sulfate as a screening test.
Cohen, LE; Denufrio, D; Dorsey, MJ; Phipatanakul, W; Schneider, LC, 2006
)
1.27
"Dehydroepiandrosterone sulfate (DHEAS) is an endogenously produced sex steroid that has been hypothesized to have anti-aging effects. "( DHEAS levels and mortality in disabled older women: the Women's Health and Aging Study I.
Cappola, AR; Ferrucci, L; Fried, LP; Guralnik, J; Leng, SX; Walston, JD; Xue, QL, 2006
)
1.78
"Dehydroepiandrosterone sulfate (DHEAS) is an excitatory neurosteroid with anti-glucocorticoid properties. "( Influence of naltrexone administration on dehydroepiandrosterone sulfate levels in male and female participants.
al'Absi, M; Ceballos, NA; France, CR, 2007
)
2.05
"Dehydroepiandrosterone sulfate (DHEAS) is a neuroactive neurosteroid."( DHEAS repeated treatment improves cognitive and behavioral deficits after mild traumatic brain injury.
Maayan, R; Milman, A; Pick, CG; Weizman, R; Zohar, O, 2008
)
1.07
"Dehydroepiandrosterone sulfate (DHEAS) is a hormone produced by the adrenal gland and is a precursor for both androgens and estrogens. "( Inhibition of vascular inflammation by dehydroepiandrosterone sulfate in human aortic endothelial cells: roles of PPARalpha and NF-kappaB.
Altman, R; Kota, RS; Motton, DD; Rutledge, JC,
)
1.84
"Dehydroepiandrosterone sulfate (DHEAS) is an endogenous steroid having a wide variety of biological effects, but its physiological role remains undefined. "( Effects of dehydroepiandrosterone sulfate on cellular calcium responsiveness and vascular contractility.
Barbagallo, M; Pang, PK; Resnick, LM; Shan, J, 1995
)
2.12
"Dehydroepiandrosterone sulfate (DHEAS) is an adrenal steroid which has been inversely associated with development of atherosclerosis. "( Quantitative genetics of dehydroepiandrosterone sulfate and its relation to possible cardiovascular disease risk factors in Mexican Americans.
Blangero, J; Haffner, SM; Jaquish, CE; Maccluer, JW; Stern, MP,
)
1.88
"Dehydroepiandrosterone sulfate (DHEAS) is a neurosteroid which functions as a negative allosteric modulator of the GABA(A) receptor-gated chloride channel. "( Chronic steroid sulfatase inhibition by (p-O-sulfamoyl)-N-tetradecanoyl tyramine increases dehydroepiandrosterone sulfate in whole brain.
Boni, RL; Johnson, DA; Li, PK; Rhodes, ME, 1997
)
1.96
"Dehydroepiandrosterone sulfate (DHEAS) is a major secretory product of the adrenal glands. "( Distribution of dehydroepiandrosterone sulfate and relationships between its level and serum lipid levels in a rural Japanese population.
Okamoto, K, 1998
)
2.09
"Dehydroepiandrosterone sulfate (DHEAS) is a neuroactive steroid with antagonist action at gamma-aminobutyric acid type A (GABAA) receptors. "( Differential blockade of gamma-aminobutyric acid type A receptors by the neuroactive steroid dehydroepiandrosterone sulfate in posterior and intermediate pituitary.
Fjalland, B; Hansen, SL; Jackson, MB, 1999
)
1.97

Effects

Dehydroepiandrosterone sulfate (DHEAS) has been reported to improve memory in aged animals and suggested as a treatment for age-related dementias. The hormone has known anti-glucocorticoid effects and may counter the effects of cortisol.

ExcerptReferenceRelevance
"Dehydroepiandrosterone sulfate (DHEAS) has known anti-glucocorticoid effects and may counter the effects of cortisol."( Persisting neuropsychiatric symptoms, Alzheimer's disease, and cerebrospinal fluid cortisol and dehydroepiandrosterone sulfate.
Clark, C; Kirschbaum, C; Ouanes, S; Popp, J; Rabl, M, 2022
)
1.66
"Dehydroepiandrosterone sulfate (DHEAS) has been proposed as an antiaging hormone, but its importance is unclear. "( Trajectories of dehydroepiandrosterone sulfate predict mortality in older adults: the cardiovascular health study.
Bartz, TM; Cappola, AR; Fried, LP; Guo, W; Newman, AB; O'Meara, ES, 2009
)
2.14
"Dehydroepiandrosterone sulfate (DHEAS) has been reported to improve memory in aged animals and suggested as a treatment for age-related dementias. "( DHEAS improves learning and memory in aged SAMP8 mice but not in diabetic mice.
Banks, WA; Farr, SA; Gaskin, FS; Morley, JE; Uezu, K, 2004
)
1.77
"Dehydroepiandrosterone sulfate (DHEAS) has well characterized effects on memory and cognitive performances. "( Chronic DHEAS administration facilitates hippocampal long-term potentiation via an amplification of Src-dependent NMDA receptor signaling.
Chen, L; Dai, XN; Furuya, K; Miyamoto, Y; Mori, N; Sokabe, M, 2006
)
1.78
"Dehydroepiandrosterone sulfate (DHEAS) has been shown to enhance memory retention in different animal models and in various learning paradigms. "( Temporal effects of dehydroepiandrosterone sulfate on memory formation in day-old chicks.
Fry, JP; Mileusnic, R; Rose, SP; Sujkovic, E, 2007
)
2.11
"Dehydroepiandrosterone sulfate (DHAS) has been measured by radioimmunoassay in 100 breast cyst fluids obtained from 82 women. "( Androgen conjugates in human breast cyst fluids.
Creel, RJ; Forrest, AP; Kelly, RW; Miller, WR; Roberts, MM; Yap, PL, 1982
)
1.71
"Dehydroepiandrosterone sulfate (DHEA-S) has been suggested as the possible link between these two entities."( Relationship between insulin sensitivity and dehydroepiandrosterone sulfate in patients with ischemic heart disease.
de Teresa, ML; Escobar-Jiménez, F; García-Robles, R; Novo, E; Piédrola, G; Serrano-Gotarredona, J, 1997
)
1.28
"Dehydroepiandrosterone sulfate levels have been inversely related with cardiovascular mortality in men, but findings have been inconsistent, and there are few data in women. "( Dehydroepiandrosterone sulfate and mortality in elderly men and women.
Khaw, KT; Trivedi, DP, 2001
)
3.2
"Dehydroepiandrosterone sulfate (DHAS) has been shown to promote cervical ripening. "( Dehydroepiandrosterone sulfate and induction of labor.
Ishikawa, M; Shimizu, T, 1989
)
3.16

Actions

DHA-S plays a critical role in cervical dilatation at labor. Dehydroepiandrosterone sulfate prevented the increase in corticosterone level.

ExcerptReferenceRelevance
"Dehydroepiandrosterone sulfate prevented the increase in corticosterone level in rats induced by repeated exposure to stress. "( Stress-limiting effect of dehydroepiandrosterone sulfate and its mechanism.
Cherkasova, OP; Obut, TA; Ovsyukova, MV, 2003
)
2.06
"Dehydroepiandrosterone sulfate (DHA-S) plays a critical role in cervical dilatation at labor. "( Dehydroepiandrosterone sulfate-binding sites in plasma membrane from human uterine cervical fibroblasts.
Imai, A; Ohno, T; Tamaya, T, 1992
)
3.17

Treatment

Dehydroepiandrosterone sulfate treatment stimulated the production of 6-keto PGF1 alpha in the cervix. Treatment significantly increased the [3H]MK801 binding sites in hippocampal areas (field CA1, CA3, dentate gyrus lateral blade and medial blade) and in cortex layer IV.

ExcerptReferenceRelevance
"Dehydroepiandrosterone sulfate treatment for 5 consecutive days from the 20th day of gestation stimulated the production of 6-keto PGF1 alpha in the cervix."( [Role of prostaglandin I2 (prostacyclin) on the maturation of human and rabbit uterine cervix].
Tanaka, M, 1984
)
0.99
"Dehydroepiandrosterone sulfate treatment significantly increased the [3H]MK801 binding sites in hippocampal areas (field CA1, CA3, dentate gyrus lateral blade and medial blade) and in cortex layer IV as compared to the control group."( Treatment with dehydroepiandrosterone sulfate increases NMDA receptors in hippocampus and cortex.
Dong, K; Onolfo, JP; Vincens, M; Wen, S, 2001
)
1.38

Toxicity

ExcerptReferenceRelevance
"These data suggest that both therapies were similarly effective and safe in the treatment of hirsutism."( Comparison of the clinical efficacy and safety of flutamide versus flutamide plus an oral contraceptive in the treatment of hirsutism.
Başogul, O; Inal, M; Ispahi, C; Karanfil, C; Onoglu, A; Taner, C; Tinar, S, 2002
)
0.31

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic parameter estimates were calculated by noncompartmental methods."( Sex differences in the pharmacokinetics of dehydroepiandrosterone (DHEA) after single- and multiple-dose administration in healthy older adults.
Folan, M; Frye, RF; Hakala, C; Kroboth, FJ; Kroboth, PD; Linares, AM; Pollock, BG; Salek, FS; Stone, RA, 2000
)
0.31
" Pharmacokinetic parameters of prednisolone as assessed by Cmax, t 1/2, AUC, or serum protein binding were not affected by prasterone."( Effects of oral prasterone (dehydroepiandrosterone) on single-dose pharmacokinetics of oral prednisone and cortisol suppression in normal women.
Blum, RA; Jusko, WJ; Meno-Tetang, GM; Schwartz, KE, 2001
)
0.31
" The glucocorticoid induced a rapid suppression of serum cortisol, DHEA, and DHEA-sulfate (DHEA-S) as well as their metabolites, thus permitting to use this model to study the pharmacokinetic parameters of DHEA and its metabolites without significant interference by endogenous steroid levels."( Bioavailability and pharmacokinetics of dehydroepiandrosterone in the cynomolgus monkey.
Bélanger, A; Candas, B; Labrie, C; Labrie, F; Leblanc, M, 2003
)
0.32
"A prospective, randomized, double-blind, placebo-controlled pharmacokinetic study."( Pharmacokinetics of dehydroepiandrosterone and its metabolites after long-term daily oral administration to healthy young men.
Acacio, BD; Jafarian, N; Mullin, P; Saadat, P; Sokol, RZ; Stanczyk, FZ, 2004
)
0.32
" No significant changes were observed in pharmacokinetic values."( Pharmacokinetics of dehydroepiandrosterone and its metabolites after long-term daily oral administration to healthy young men.
Acacio, BD; Jafarian, N; Mullin, P; Saadat, P; Sokol, RZ; Stanczyk, FZ, 2004
)
0.32

Compound-Compound Interactions

ExcerptReferenceRelevance
" In the postmenopausal women the plasma levels of IGF-I, gonadotrophins and sex hormones were determined before and after 3 and 6 months cyclic replacement therapy with transdermal 17 beta-estradiol (E2 100 micrograms patches applied twice weekly) combined with oral chlormadinone acetate (2 mg daily for 7 days in each cycle)."( Transdermal 17 beta-estradiol combined with oral progestogen increases plasma levels of insulin-like growth factor-I in postmenopausal women.
Brzezinska, A; Jeske, W; Sadowski, Z; Slowinska-Srzednicka, J; Srzednicki, M; Stopinska-Gluszak, U; Zgliczynski, S; Zgliczynski, W,
)
0.13
"Since drug-drug interaction (DDI) can affect organic anion-transporting polypeptide (OATP) and cause clinical events, prediction of such DDI is important in early clinical development."( Dehydroepiandrosterone sulfate, a useful endogenous probe for evaluation of drug-drug interaction on hepatic organic anion transporting polypeptide (OATP) in cynomolgus monkeys.
Tamai, I; Watanabe, M; Watanabe, T; Yabuki, M, 2015
)
1.86

Bioavailability

ExcerptReferenceRelevance
"Because dehydroepiandrosterone may protect against neoplasia, osteoporosis, and cardiac disease, we investigated the bioavailability of oral micronized dehydroepiandrosterone, anticipating its adjunctive use in postmenopausal steroid replacement."( Postmenopausal steroid replacement with micronized dehydroepiandrosterone: preliminary oral bioavailability and dose proportionality studies.
Abraham, GE; Buster, JE; Casson, PR; Chiamori, N; Dale, D; Straughn, AB; Umstot, ES, 1992
)
0.28
"To demonstrate bioavailability of 3 weeks of oral micronized DHEA and to delineate changes induced on insulin sensitivity, morphometric indexes, and lipoprotein profiles."( Replacement of dehydroepiandrosterone enhances T-lymphocyte insulin binding in postmenopausal women.
Abraham, GE; Andersen, RN; Buster, JE; Casson, PR; Faquin, LC; Stentz, FB; Straughn, AB, 1995
)
0.29
" However, the study cohort appeared to consist of two subpopulations with markedly different bioavailability for a given DHEA dose."( An open-label dose-escalation trial of oral dehydroepiandrosterone tolerance and pharmacokinetics in patients with HIV disease.
Dyner, TS; Galmarini, M; Geaga, J; Golub, A; Jacobson, MA; Lang, W; Masterson, J; Stites, D; Winger, E, 1993
)
0.29
" Adrenal steroids may serve as endocrine regulators of androgen bioavailability and bioactivity."( Endocrine interactions: adrenal steroids and precursors.
Pitha, J; Scherrer, J; Taylor, GT; Weiss, J, 1994
)
0.29
" Taking the bioavailability obtained by the subcutaneous route as 100%, it is estimated that the potencies of DHEA by the percutaneous and oral routes are approximately 33 and 3% respectively."( High bioavailability of dehydroepiandrosterone administered percutaneously in the rat.
Bélanger, A; Flamand, M; Labrie, C; Labrie, F, 1996
)
0.29
" Accordingly, we measured levels of IGFBP-1, an important short term modulator of IGF bioavailability that is suppressed by insulin, and levels of IGFBP-3, the major circulating IGF carrier protein, and examined their relationships to insulin, glucose, IGF, and dehydroepiandrosterone sulfate levels and anthropometric measures in old (63-89 yr) and young (23-39 yr) men."( Circulating levels of insulin-like growth factor (IGF) binding protein-1 and -3 in aging men: relationships to insulin, glucose, IGF, and dehydroepiandrosterone sulfate levels and anthropometric measures.
Benbassat, CA; Maki, KC; Unterman, TG, 1997
)
0.68
" Despite decreased IGF-I levels, target final height was attained, probably because of adequate insulin compensation leading to normal IGFBP-l, thus adequate bioavailability of IGF-I."( Determinants of growth in diabetic pubertal subjects.
Brismar, K; Dahlqvist, G; Hall, K; Wallensteen, M; Zachrisson, I, 1997
)
0.3
" It was found that DHEA is well absorbed and rapidly metabolized to its sulfate (DHEAS), androstenedione, and consequently to testosterone and estradiol."( Effects of transdermal application of DHEA on the levels of steroids, gonadotropins and lipids in men.
Ceska, R; Hampl, R; Hill, M; Masek, Z; Novácek, A; Stárka, L; Sulcová, J, 2000
)
0.31
" The impact of aging and of estrogen replacement therapy, particularly oral ERT, significantly reduces androgen bioavailability after menopause."( Estrogen replacement therapy: effects on the endogenous androgen milieu.
Simon, JA, 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
" Therefore, the bioavailability of estradiol in the oldest men was likely diminished."( Testicular and blood steroid levels in aged men.
Bourguiba, S; Carreau, S; Marie, E, 2004
)
0.32
" Mechanical wounding reduced fibroblast aromatase activity but increased keratinocyte activity, amplifying the bioavailability of intracellular estrogen."( Intracrine sex steroid synthesis and signaling in human epidermal keratinocytes and dermal fibroblasts.
Colombo, L; Dalla Valle, L; Pertile, P; Pomari, E; Thornton, MJ, 2015
)
0.42
"There is an abnormal increase in TGF-β1 bioavailability in women with polycystic ovary syndrome (PCOS), which might play a role in the pathophysiology of this syndrome."( Vitamin D Supplementation Decreases TGF-β1 Bioavailability in PCOS: A Randomized Placebo-Controlled Trial.
Bhatt, D; Grazi, RV; Irani, M; Irani, S; Julka, N; Kalgi, B; Lambert-Messerlian, G; Seifer, DB; Tal, O; Tal, R, 2015
)
0.42
"The objective of the study was to determine the effect of VD supplementation on TGF-β1 bioavailability in VD-deficient women with PCOS and assess whether changes in TGF-β1/soluble endoglin (sENG) levels correlate with an improvement in PCOS clinical manifestations."( Vitamin D Supplementation Decreases TGF-β1 Bioavailability in PCOS: A Randomized Placebo-Controlled Trial.
Bhatt, D; Grazi, RV; Irani, M; Irani, S; Julka, N; Kalgi, B; Lambert-Messerlian, G; Seifer, DB; Tal, O; Tal, R, 2015
)
0.42
"VD supplementation in VD-deficient women with PCOS significantly decreases the bioavailability of TGF-β1, which correlates with an improvement in some abnormal clinical parameters associated with PCOS."( Vitamin D Supplementation Decreases TGF-β1 Bioavailability in PCOS: A Randomized Placebo-Controlled Trial.
Bhatt, D; Grazi, RV; Irani, M; Irani, S; Julka, N; Kalgi, B; Lambert-Messerlian, G; Seifer, DB; Tal, O; Tal, R, 2015
)
0.42
"Overall, vitamin D was associated with sex hormone-binding globulin and free androgen index in eumenorrheic women with prior pregnancy loss, suggesting that vitamin D may play a role in the bioavailability of androgens in eumenorrheic women."( Vitamin D is associated with bioavailability of androgens in eumenorrheic women with prior pregnancy loss.
Alkhalaf, Z; Connell, MT; Holland, TL; Kim, K; Kuhr, DL; Mumford, SL; Omosigho, UR; Perkins, NJ; Plowden, TC; Schisterman, EF; Silver, RM; Sjaarda, LA, 2018
)
0.48

Dosage Studied

We investigated the dose-response relationship for suppression of dehydroepiandrosterone sulfate (DHEAS) with the use of dexamethasone. EM-1913 partially (26%) and almost entirely blocked the stimulating effect of DHEAS on ventral prostates and seminal vesicles.

ExcerptRelevanceReference
"40 with a suggestion of a dose-response trend with increasing levels."( Relationship of prediagnostic serum levels of dehydroepiandrosterone and dehydroepiandrosterone sulfate to the risk of developing premenopausal breast cancer.
Alberg, AJ; Bush, TL; Comstock, GW; Gordon, GB; Helzlsouer, KJ, 1992
)
0.52
" We investigated the dose-response relationship for suppression of dehydroepiandrosterone sulfate (DHEAS) with the use of dexamethasone."( Treatment of androgenic disorders with dexamethasone: dose-response relationship for suppression of dehydroepiandrosterone sulfate.
Bedocs, NM; Bergfeld, W; Gidwani, GP; Gupta, MK; Parker, R; Redmond, GP; Skibinski, C, 1990
)
0.73
" These data demonstrate a consistent, independent, inverse, dose-response relation between plasma DHEA sulfate levels and angiographically defined coronary atherosclerosis in men."( Plasma dehydroepiandrosterone and dehydroepiandrosterone sulfate in patients undergoing diagnostic coronary angiography.
Achuff, SC; Gordon, GB; Herrington, DM; Kwiterovich, PO; Pearson, TA; Trejo, JF; Weisman, HF, 1990
)
0.56
" Prednisolone was given in a dosage averaging 25 mg at 12 h intervals orally for up to 2 weeks to adult volunteers."( Recovery from glucocorticoid inhibition of the responses to corticotrophin-releasing hormone.
Fang, VS; Rosenfield, RL; Watson, AC, 1988
)
0.27
" Anatomical variations and collateral flow as well as stress effects and the dosage of contrast media were studied."( Technical difficulties of selective venous blood sampling in the differential diagnosis of female hyperandrogenism.
Moltz, L; Schwartz, U; Sörensen, R, 1986
)
0.27
" A dose-response relation was apparent for these hormones; mean plasma levels increased concomitantly with cigarette consumption."( Cigarette smoking and levels of adrenal androgens in postmenopausal women.
Barrett-Connor, E; Khaw, KT; Tazuke, S, 1988
)
0.27
" Side-effects are frequent, possibly as a result of the high dosage used in this study."( Clinical and endocrine effects of cyproterone acetate in postmenopausal patients with advanced breast cancer.
de Vries, EG; Dikkeschei, LD; Mulder, NH; Sleijfer, DT; van der Ploeg, E; Willemse, PH, 1988
)
0.27
" Prednisolone therapy in 22 patients (mean dosage 8 mg/day) was associated with reductions in estrone and testosterone levels; however, DHEAS and femoral BMD were also decreased in RA patients who were not receiving corticosteroids."( Sex hormone status and osteoporosis in postmenopausal women with rheumatoid arthritis.
Champion, GD; Eisman, JA; Pocock, NA; Sambrook, PN, 1988
)
0.27
"To test the hypothesis that adrenal androgen secretion is more easily suppressed than is cortisol secretion by glucocorticoids, we examined the dose-response relationship for suppression of serum dehydroepiandrosterone (DHA), DHA sulfate (DHAS), testosterone, and cortisol by dexamethasone."( Sensitivity of cortisol and adrenal androgens to dexamethasone suppression in hirsute women.
Cutler, GB; Loriaux, DL; Rittmaster, RS, 1985
)
0.27
" LH-FSH basal levels, prolactin, TSH, TBG, thyroxine, cortisol, and androstenedione were not changed by either dosage or duration of danazol therapy."( Danazol: endocrine and endometrial effects.
Floyd, WS, 1980
)
0.26
" These results show that a low intravenous dosage of betamethason and collection of blood samples for E3 assays in intervals of 12 hours can be used as a functional test of the fetoplacental unit."( [The betamethasone test in the diagnosis of placental insufficiency].
Bernaschek, G; Bieglmayer, C; Friedrich, F, 1983
)
0.27
" Side-effects were less at the lowest dosage and were age-related."( Aminoglutethimide dose and hormone suppression in advanced breast cancer.
Dowsett, M; Harris, AL; Jeffcoate, SL; Smith, IE, 1983
)
0.27
"In a randomized, double-blind, dose-response study, alpha-tocopherol significantly ameliorated symptoms in three of the four classes of the premenstrual syndrome (PMS)."( The effect of alpha-tocopherol on premenstrual symptomatology: a double-blind study. II. Endocrine correlates.
Goldstein, P; London, RS; Manimekalai, S; Murphy, L; Reynolds, M; Sundaram, G, 1984
)
0.27
" Pregnant rats groups were given the drugs on the 19th day of gestation at dosage of 10, 20 and 40 mg/kg respectively."( [Ripening effect of mylis and tiluoan on the uterine cervix in pregnant rats].
Shi, SQ; Zuo, XC; Zuo, Z, 1994
)
0.29
" Dose proportionality was evidenced neither by the serum DHEA nor by DHEA-S time-concentration curves for the three dosing groups."( An open-label dose-escalation trial of oral dehydroepiandrosterone tolerance and pharmacokinetics in patients with HIV disease.
Dyner, TS; Galmarini, M; Geaga, J; Golub, A; Jacobson, MA; Lang, W; Masterson, J; Stites, D; Winger, E, 1993
)
0.29
" Although mean levels of DHEA were 11% lower among cases than controls and DHEA-S levels were 12% lower than among controls, no dose-response association was noted for either DHEA or DHEA-S."( The relationship of serum dehydroepiandrosterone and its sulfate to subsequent cancer of the prostate.
Comstock, GW; Gordon, GB; Hsing, AW,
)
0.13
" Only mice immunized shortly after oral dosing with DHEAS demonstrated high serum antibody titers and complete protection from paralysis."( DHEAS as an effective vaccine adjuvant in elderly humans. Proof-of-principle studies.
Araneo, B; Daynes, R; Dowell, T; Evans, T; Judd, M; Woods, ML, 1995
)
0.29
" However, because the gene for steroid sulphatase activity partly escapes from the process of X-chromosome inactivation associated with gene dosage compensation, identification of heterozygotes (females) is more difficult."( Steroid sulphatase deficiency: identification of heterozygotes using hydrolysis of dehydroepiandrosterone sulphate by peripheral leucocytes.
Lowis, EI; Oakey, RE, 1996
)
0.29
" The patients were orally treated with an initial dosage of 50 mg acarbose/ day, which was gradually increased to a maximum of 300 mg/day."( Acarbose reduces elevated testosterone serum concentrations in hyperinsulinaemic premenopausal women: a pilot study.
Brabant, G; Frorath, B; Geisthövel, F, 1996
)
0.29
" Quantitative analysis by gas chromatography-mass spectrometry with selected ion monitoring demonstrated that the drug was readily absorbed with 50 to 75% recovery of dosing after 24 h, and with glucuro- and sulfoconjugates of DHEA, androsterone, and etiocholanolone as the most abundant metabolites."( Oral administration of dehydroepiandrosterone to healthy men: alteration of the urinary androgen profile and consequences for the detection of abuse in sport by gas chromatography-mass spectrometry.
Dehennin, L; Ferry, M; Lafarge, JP; Lafarge, P; Pérès, G, 1998
)
0.3
"We used 2 dosage levels of postoperative opioid administration to determine whether the degree of postoperative analgesia after laparotomy during the last third of baboon pregnancy alters maternal pituitary-adrenal function, androgen secretion, and placental estrogen production."( Level of postoperative analgesia is a critical factor in regulation of myometrial contractility after laparotomy in the pregnant baboon: implications for human fetal surgery.
Abrams, LM; Ding, XY; Giussani, DA; Nathanielsz, PW; Tame, JD; Yen, A, 1999
)
0.3
" The high CEE dosage in group 3 resulted in a significant increase of TG and decrease of Lp(a) and PAI-1."( The effects of six months of treatment with a low-dose of conjugated oestrogens in menopausal women.
Ebert, C; Junker, R; Petersdorf, LI; Schlegel, W; Schulte, H; Von Eckardstein, A, 1999
)
0.3
"This study sought to determine effects of multiple dosing of prasterone (DHEA, dehydroepiandrosterone) on the pharmacokinetics of prednisolone and endogenous cortisol secretion."( Effects of oral prasterone (dehydroepiandrosterone) on single-dose pharmacokinetics of oral prednisone and cortisol suppression in normal women.
Blum, RA; Jusko, WJ; Meno-Tetang, GM; Schwartz, KE, 2001
)
0.31
"Two XY female adolescents with 17-hydroxylase deficiency and 2 XX females with panhypopituitarism presenting with atrichia pubis were treated with a daily dosage of DHEAS 10 mg/m2 body surface in addition to their regular substitution therapy."( Dehydroepiandrosterone sulfate treatment for atrichia pubis.
Jansen, M; Langenhorst, VJ; Oostdijk, WA; van Doorn, J; Wit, JM, 2001
)
1.75
"A dosage of 10 mg/m2 for 1 year led to serum DHEAS levels at the lower limit of the normal range."( Dehydroepiandrosterone sulfate treatment for atrichia pubis.
Jansen, M; Langenhorst, VJ; Oostdijk, WA; van Doorn, J; Wit, JM, 2001
)
1.75
" In cases of inadequate dosage there were side effects like sleepiness,restlessness, headache, acne/hirsutism, effluvium or odors in a percentage of 34, 17, 9, 31, 21 and 11% of the women, respectively."( [Adrenopause and dehydroepiandrosterone: pharmacological therapy versus replacement therapy].
Römmler, A, 2003
)
0.32
" A defined soy protein amount per day (20 g) with a low dosage of isoflavones (20 mg) was used."( Effect of soy supplementation on endogenous hormones in postmenopausal women.
Foth, D; Nawroth, F, 2003
)
0.32
" After 1 yr of GH treatment, the increase of serum DHEAS levels was the same for both GH dosage groups and the untreated group."( Serum dehydroepiandrosterone sulfate levels and pubarche in short children born small for gestational age before and during growth hormone treatment.
Boonstra, VH; de Jong, FH; Hokken-Koelega, AC; Mulder, PG, 2004
)
0.8
"A 14-day oral administration of a widely used, standardized ginkgo extract at a generally advocated dosage of 240 mg/day did not significantly alter concentrations of major circulating steroids in men and women."( Effect of Ginkgo biloba extract on plasma steroid concentrations in healthy volunteers: a pilot study.
Chavin, KD; DeVane, CL; Donovan, JL; Lewis, JG; Markowitz, JS; Wang, JS, 2005
)
0.33
"03), without any dose-response relationship."( Effects of raloxifene on sex steroid hormones and C-telopeptide in postmenopausal women with primary breast cancer.
Baglietto, L; Bonanni, B; Cazzaniga, M; Decensi, A; Guerrieri-Gonzaga, A; Johansson, H; Luini, A; Mariette, F; Pelosi, G; Sandri, MT, 2006
)
0.33
"All randomized placebo-controlled trials enrolling people aged over 50 without dementia and to whom DHEA/S in any dosage was administered for more than one day were considered for inclusion in the review."( Dehydroepiandrosterone (DHEA) supplementation for cognitive function in healthy elderly people.
Grimley Evans, J; Huppert, F; Malouf, R; van Niekerk, JK, 2006
)
0.33
" The present results suggest that there is a dose-response relationship between increased training load, resting DHEA-S/C ratio and subjective assessment of stress and recovery, implying that this ratio could be used as an indicator of training status in female athletes."( Relationships among training stress, mood and dehydroepiandrosterone sulphate/cortisol ratio in female cyclists.
Bouget, M; Filaire, E; Michaux, O; Pequignot, JM; Rouveix, M, 2006
)
0.33
"Although further long-term studies of DHEA therapy, with dosage adjustment, are desirable, our results support some beneficial effects of prolonged DHEA treatment in Addison's disease."( Long-term DHEA replacement in primary adrenal insufficiency: a randomized, controlled trial.
Chatterjee, VK; Compston, JE; Conway, CL; Curran, SE; Gurnell, EM; Herbert, J; Hunt, PJ; Huppert, FA; Pullenayegum, EM, 2008
)
0.35
" Clinically, the spectrum of women that would benefit from DHEA therapy is not clearly defined and nor is the dosage of hormone treatment."( DHEA therapy in postmenopausal women: the need to move forward beyond the lack of evidence.
Genazzani, AR; Pluchino, N, 2010
)
0.36
" Clinical trials for the evaluation of these neurosteroids face challenges in terms of experimental design, dosing strategy, data analysis, and interpretation."( The clinical and therapeutic potentials of dehydroepiandrosterone and pregnenolone in schizophrenia.
Ritsner, MS, 2011
)
0.37
" After determining the required dosage of dehydroepiandrosterone sulfate (DHEAS) needed to stimulate the ventral prostate and seminal vesicles in castrated rats, we measured that EM-1913 partially (26%) and almost entirely blocked (81%) the stimulating effect of DHEAS on ventral prostates and seminal vesicles, respectively."( Inhibition of dehydroepiandosterone sulfate action in androgen-sensitive tissues by EM-1913, an inhibitor of steroid sulfatase.
Lefebvre, J; Maltais, R; Poirier, D; Roy, J, 2013
)
0.65
" If an association was found, we further explored dose-response relationships by the number of pain locations and the degree of pain interference."( Blood Dehydroepiandrosterone and Dehydroepiandrosterone Sulfate as Pathophysiological Correlates of Chronic Pain: Analyses Using a National Sample of Midlife Adults in the United States.
Chapman, BP; Li, R; Smith, SM, 2021
)
0.9
" DHEA dosing has increased to 100 mg in both male cohorts and remains on 50 mg in across all female groups."( A prospective, phase II, single-centre, cross-sectional, randomised study investigating Dehydroepiandrosterone supplementation and its Profile in Trauma: ADaPT.
Arlt, W; Athwal, A; Barton, D; Bentley, C; Brock, K; Carrera, R; Desai, A; Ermogenous, C; Foster, MA; Gilligan, LC; Greig, CA; Hazeldine, J; Homer, V; Lord, JM; McGee, K; Potter, C; Shaheen, F; Sur, G; Taylor, AE; Toman, E; Yakoub, KM; Young, K, 2021
)
0.62
" We also conducted a dose-response meta-analysis of prospective studies of circulating estrone and estradiol with colorectal, colon, and rectal cancer risk in postmenopausal women."( Endogenous Circulating Sex Hormone Concentrations and Colon Cancer Risk in Postmenopausal Women: A Prospective Study and Meta-Analysis.
Ardanaz, E; Aune, D; Bueno-de-Mesquita, B; Colorado-Yohar, SM; Cross, AJ; Dimou, N; Fortner, RT; Fournier, A; Gicquiau, A; Gram, IT; Gunter, MJ; Harbs, J; Harlid, S; Jakszyn, P; Kaaks, R; Keski-Rahkonen, P; Krogh, V; Kvaskoff, M; Masala, G; Mori, N; Murphy, N; Panico, S; Rinaldi, S; Sacerdote, C; Sánchez, MJ; Schulze, MB; Severi, G; Travis, R; Tsilidis, KK; Tumino, R; Van Guelpen, B; Waaseth, M; Watts, EL, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
EC 2.7.1.33 (pantothenate kinase) inhibitorAn EC 2.7.1.* (phosphotransferases with an alcohol group as acceptor) inhibitor that interferes with the action of pantothenate kinase (EC 2.7.1.33).
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
mouse metaboliteAny mammalian metabolite produced during a metabolic reaction in a mouse (Mus musculus).
[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 (2)

ClassDescription
steroid sulfateA sulfuric ester obtained by the formal condensation of a hydroxy group of any steroid with sulfuric acid.
17-oxo steroidAny oxo steroid carrying the oxo group at position 17.
[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 (5)

PathwayProteinsCompounds
Androgen and Estrogen Metabolism1230
17-beta Hydroxysteroid Dehydrogenase III Deficiency1230
Aromatase Deficiency1230
Sulfatase and aromatase pathway1414
Biochemical pathways: part I0466

Protein Targets (15)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)3.00000.20005.677410.0000AID681920
[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)
G-protein coupled bile acid receptor 1Homo sapiens (human)EC50 (µMol)127.00000.02372.52598.9000AID324923
[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)
Multidrug resistance-associated protein 4Homo sapiens (human)Km1.90001.90004.27259.6900AID681877
Solute carrier organic anion transporter family member 1A4Rattus norvegicus (Norway rat)Km17.00000.24003.28416.5300AID681364
Solute carrier organic anion transporter family member 1A5Rattus norvegicus (Norway rat)Km162.00004.30006.39608.8000AID681149
Steryl-sulfataseHomo sapiens (human)Km10.35000.80001.25001.7000AID205784; AID205786
Multidrug resistance-associated protein 1 Homo sapiens (human)Km5.00000.73002.65505.0000AID681072
Solute carrier organic anion transporter family member 1A1Rattus norvegicus (Norway rat)Km5.00000.01503.49967.0000AID682135
Solute carrier organic anion transporter family member 1A2Homo sapiens (human)Km6.60006.40007.42009.6000AID682075
Solute carrier organic anion transporter family member 1A3Rattus norvegicus (Norway rat)Km8.05001.00004.43338.5000AID681577; AID681578
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Km30.00000.03912.93886.4000AID681593
Solute carrier family 22 member 11Homo sapiens (human)Km0.63000.15400.62151.0100AID678971
Solute carrier organic anion transporter family member 1A1Mus musculus (house mouse)Km8.20005.00007.13338.2000AID679643
Solute carrier organic anion transporter family member 1B2Rattus norvegicus (Norway rat)Km5.30001.10005.28339.4500AID681150
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)Km21.50000.00763.201810.0000AID681365
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (49)

Processvia Protein(s)Taxonomy
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
steroid catabolic processSteryl-sulfataseHomo sapiens (human)
female pregnancySteryl-sulfataseHomo sapiens (human)
epidermis developmentSteryl-sulfataseHomo sapiens (human)
leukotriene metabolic processMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 1 Homo sapiens (human)
response to xenobiotic stimulusMultidrug resistance-associated protein 1 Homo sapiens (human)
cobalamin transportMultidrug resistance-associated protein 1 Homo sapiens (human)
sphingolipid biosynthetic processMultidrug resistance-associated protein 1 Homo sapiens (human)
cellular response to oxidative stressMultidrug resistance-associated protein 1 Homo sapiens (human)
heme catabolic processMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic transportMultidrug resistance-associated protein 1 Homo sapiens (human)
phospholipid translocationMultidrug resistance-associated protein 1 Homo sapiens (human)
positive regulation of inflammatory responseMultidrug resistance-associated protein 1 Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
cell chemotaxisMultidrug resistance-associated protein 1 Homo sapiens (human)
transepithelial transportMultidrug resistance-associated protein 1 Homo sapiens (human)
cyclic nucleotide transportMultidrug resistance-associated protein 1 Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 1 Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
sphingolipid translocationMultidrug resistance-associated protein 1 Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 1 Homo sapiens (human)
cellular response to amyloid-betaMultidrug resistance-associated protein 1 Homo sapiens (human)
carboxylic acid transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierMultidrug resistance-associated protein 1 Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic metabolic processSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
monoatomic ion transportSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
organic cation transportSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
organic anion transportSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
bile acid and bile salt transportSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
cell surface bile acid receptor signaling pathwayG-protein coupled bile acid receptor 1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeG-protein coupled bile acid receptor 1Homo sapiens (human)
cellular response to bile acidG-protein coupled bile acid receptor 1Homo sapiens (human)
positive regulation of cholangiocyte proliferationG-protein coupled bile acid receptor 1Homo sapiens (human)
regulation of bicellular tight junction assemblyG-protein coupled bile acid receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayG-protein coupled bile acid receptor 1Homo sapiens (human)
organic anion transportATP-binding cassette sub-family C member 11Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 11Homo sapiens (human)
purine nucleotide transportATP-binding cassette sub-family C member 11Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 11Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 11Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 11Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 11Homo sapiens (human)
xenobiotic metabolic processSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
monoatomic ion transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
organic anion transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
bile acid and bile salt transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
heme catabolic processSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
monoatomic ion transportSolute carrier family 22 member 11Homo sapiens (human)
inorganic anion transportSolute carrier family 22 member 11Homo sapiens (human)
organic anion transportSolute carrier family 22 member 11Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 11Homo sapiens (human)
urate metabolic processSolute carrier family 22 member 11Homo sapiens (human)
transmembrane transportSolute carrier family 22 member 11Homo sapiens (human)
xenobiotic metabolic processSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
monoatomic ion transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
organic anion transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
bile acid and bile salt transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
prostaglandin transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
heme catabolic processSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
thyroid hormone transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (35)

Processvia Protein(s)Taxonomy
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
steryl-sulfatase activitySteryl-sulfataseHomo sapiens (human)
sulfuric ester hydrolase activitySteryl-sulfataseHomo sapiens (human)
metal ion bindingSteryl-sulfataseHomo sapiens (human)
arylsulfatase activitySteryl-sulfataseHomo sapiens (human)
ATP bindingMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type vitamin B12 transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATPase-coupled lipid transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
sphingolipid transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
carboxylic acid transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1A2Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier organic anion transporter family member 1A2Homo sapiens (human)
bile acid transmembrane transporter activitySolute carrier organic anion transporter family member 1A2Homo sapiens (human)
transmembrane transporter activitySolute carrier organic anion transporter family member 1A2Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1A2Homo sapiens (human)
protein bindingG-protein coupled bile acid receptor 1Homo sapiens (human)
bile acid receptor activityG-protein coupled bile acid receptor 1Homo sapiens (human)
G protein-coupled bile acid receptor activityG-protein coupled bile acid receptor 1Homo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 11Homo sapiens (human)
organic anion transmembrane transporter activityATP-binding cassette sub-family C member 11Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 11Homo sapiens (human)
purine nucleotide transmembrane transporter activityATP-binding cassette sub-family C member 11Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 11Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 11Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 11Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 11Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 11Homo sapiens (human)
serine-type endopeptidase inhibitor activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
bile acid transmembrane transporter activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
solute:inorganic anion antiporter activitySolute carrier family 22 member 11Homo sapiens (human)
protein bindingSolute carrier family 22 member 11Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 11Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 11Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier family 22 member 11Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
bile acid transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
thyroid hormone transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
lysosomeSteryl-sulfataseHomo sapiens (human)
endosomeSteryl-sulfataseHomo sapiens (human)
endoplasmic reticulumSteryl-sulfataseHomo sapiens (human)
endoplasmic reticulum lumenSteryl-sulfataseHomo sapiens (human)
endoplasmic reticulum membraneSteryl-sulfataseHomo sapiens (human)
Golgi apparatusSteryl-sulfataseHomo sapiens (human)
plasma membraneSteryl-sulfataseHomo sapiens (human)
membraneSteryl-sulfataseHomo sapiens (human)
intracellular membrane-bounded organelleSteryl-sulfataseHomo sapiens (human)
plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
basal plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
lateral plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
extracellular exosomeMultidrug resistance-associated protein 1 Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
plasma membraneSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
apical plasma membraneSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
cytoplasmG-protein coupled bile acid receptor 1Homo sapiens (human)
plasma membraneG-protein coupled bile acid receptor 1Homo sapiens (human)
receptor complexG-protein coupled bile acid receptor 1Homo sapiens (human)
plasma membraneG-protein coupled bile acid receptor 1Homo sapiens (human)
vacuolar membraneATP-binding cassette sub-family C member 11Homo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 11Homo sapiens (human)
apical plasma membraneATP-binding cassette sub-family C member 11Homo sapiens (human)
cytoplasmic vesicle membraneATP-binding cassette sub-family C member 11Homo sapiens (human)
extracellular exosomeATP-binding cassette sub-family C member 11Homo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 11Homo sapiens (human)
plasma membraneSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
plasma membraneSolute carrier family 22 member 11Homo sapiens (human)
external side of plasma membraneSolute carrier family 22 member 11Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 11Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 11Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 11Homo sapiens (human)
plasma membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (46)

Assay IDTitleYearJournalArticle
AID681595TP_TRANSPORTER: uptake in Xenopus laevis oocytes2002Biochimica et biophysica acta, Aug-19, Volume: 1564, Issue:1
Functional characterization of the mouse organic-anion-transporting polypeptide 2.
AID681920TP_TRANSPORTER: inhibition of E217betaG uptake in membrane vesicles from MRP4-expressing Sf9 cells2004The international journal of biochemistry & cell biology, Feb, Volume: 36, Issue:2
Multidrug resistance protein 4 (MRP4/ABCC4) mediates efflux of bimane-glutathione.
AID679435TP_TRANSPORTER: uptake (pH 5.0) of Dehydroepiandrosterone-3-sulfate at a concentration of 2.98 nM in OATP-B-expressing HEK293 cells2004The Journal of pharmacology and experimental therapeutics, Feb, Volume: 308, Issue:2
Functional characterization of pH-sensitive organic anion transporting polypeptide OATP-B in human.
AID1624944Substrate activity at Helix pomatia arylsulfatase assessed as enzyme-mediated compound hydrolysis using 1 U of enzyme measured after 24 hrs by UPLC-MS/MS analysis2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Comprehensive kinetic and substrate specificity analysis of an arylsulfatase from Helix pomatia using mass spectrometry.
AID681072TP_TRANSPORTER: uptake in membrane vesicles from MRP1-expressing Sf9 cells2004The international journal of biochemistry & cell biology, Feb, Volume: 36, Issue:2
Multidrug resistance protein 4 (MRP4/ABCC4) mediates efflux of bimane-glutathione.
AID681594TP_TRANSPORTER: transepithelial transport in OATP1B3/MRP2 double transfectant (MDCKII)2001Molecular pharmacology, Nov, Volume: 60, Issue:5
Vectorial transport by double-transfected cells expressing the human uptake transporter SLC21A8 and the apical export pump ABCC2.
AID324923Agonist activity at human TGR5 expressed in CHO cells by luciferase assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.
AID681593TP_TRANSPORTER: uptake in OATP8-expressing HEK293 cells2001The Journal of biological chemistry, Mar-30, Volume: 276, Issue:13
Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6.
AID588979Substrates of transporters of clinical importance in the absorption and disposition of drugs, MRP42010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID680261TP_TRANSPORTER: inhibition of Taurocholate uptake (Taurocholate: 0.5 uM, DHEAS: 50 uM) in Oatp1-expressing 293c18 cells1999The Journal of biological chemistry, Dec-24, Volume: 274, Issue:52
A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters.
AID681346TP_TRANSPORTER: ATP-dependent uptake in membrane vesicle from MRP8-expressing LLC-PK1 cells2005Molecular pharmacology, Feb, Volume: 67, Issue:2
Transport of bile acids, sulfated steroids, estradiol 17-beta-D-glucuronide, and leukotriene C4 by human multidrug resistance protein 8 (ABCC11).
AID681173TP_TRANSPORTER: uptake in Xenopus laevis oocytes2000Biochemical and biophysical research communications, Sep-07, Volume: 275, Issue:3
Molecular identification of a rat novel organic anion transporter moat1, which transports prostaglandin D(2), leukotriene C(4), and taurocholate.
AID679415TP_TRANSPORTER: uptake of DHEAS at a concentration of 17.4nM in OATP2B1-expressing HEK293 cells2005Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 33, Issue:4
Citrus juices inhibit the function of human organic anion-transporting polypeptide OATP-B.
AID682096TP_TRANSPORTER: inhibition of Pravastatin uptake (Pravastatin: 0.5 uM, DHEAS: 50 uM) in Oatp1-expressing 293c18 cells1999The Journal of biological chemistry, Dec-24, Volume: 274, Issue:52
A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters.
AID679304TP_TRANSPORTER: Transepithelial Transport (basal to apical) in OATP1B1/MRP2 double transfected LLC-PK1 cell2005Biochemical pharmacology, Feb-01, Volume: 69, Issue:3
Directional trans-epithelial transport of organic anions in porcine LLC-PK1 cells that co-express human OATP1B1 (OATP-C) and MRP2.
AID205784Michaelis-Menten constant was determined against human placental steroid sulfatase2000Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
Structure-activity relationships of 17alpha-derivatives of estradiol as inhibitors of steroid sulfatase.
AID681151TP_TRANSPORTER: uptake in Xenopus laevis oocytes2001Gastroenterology, Feb, Volume: 120, Issue:2
Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver.
AID681364TP_TRANSPORTER: uptake in Xenopus laevis oocytes1999Gastroenterology, Sep, Volume: 117, Issue:3
Localization and function of the organic anion-transporting polypeptide Oatp2 in rat liver.
AID680613TP_TRANSPORTER: inhibition of Estradiol-17beta-D-glucuronide uptake by Dehydroepiandrosterone-3-sulfate at a concentration of 10 uM in membrane vesicle from MRP8-expressing LLC-PK1 cells2005Molecular pharmacology, Feb, Volume: 67, Issue:2
Transport of bile acids, sulfated steroids, estradiol 17-beta-D-glucuronide, and leukotriene C4 by human multidrug resistance protein 8 (ABCC11).
AID679426TP_TRANSPORTER: uptake (pH 7.4) of Dehydroepiandrosterone-3-sulfate at a concentration of 2.98 nM in OATP-B-expressing HEK293 cells2004The Journal of pharmacology and experimental therapeutics, Feb, Volume: 308, Issue:2
Functional characterization of pH-sensitive organic anion transporting polypeptide OATP-B in human.
AID682135TP_TRANSPORTER: uptake in Oatp1-expressing CHO-03 cell1999The American journal of physiology, 04, Volume: 276, Issue:4
Polyspecific substrate uptake by the hepatic organic anion transporter Oatp1 in stably transfected CHO cells.
AID681172TP_TRANSPORTER: uptake (vesicle) in membrane vesicles from ABCG2-expressing P388 cells2003The Journal of biological chemistry, Jun-20, Volume: 278, Issue:25
ABCG2 transports sulfated conjugates of steroids and xenobiotics.
AID681365TP_TRANSPORTER: uptake in OATP-C-expressing HEK293 cells2001The Journal of biological chemistry, Mar-30, Volume: 276, Issue:13
Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6.
AID681141TP_TRANSPORTER: uptake in Xenopus laevis oocytes2001Molecular pharmacology, May, Volume: 59, Issue:5
Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney.
AID682075TP_TRANSPORTER: uptake in Xenopus laevis oocytes1998FEBS letters, Mar-13, Volume: 424, Issue:3
Dehydroepiandrosterone sulfate (DHEAS): identification of a carrier protein in human liver and brain.
AID681578TP_TRANSPORTER: uptake in OAT-K1-expressing MDCK cells2001The Journal of pharmacology and experimental therapeutics, Oct, Volume: 299, Issue:1
Multispecific substrate recognition of kidney-specific organic anion transporters OAT-K1 and OAT-K2.
AID679696TP_TRANSPORTER: inhibition of Taurocholate uptake (Taurocholate: 0.25 uM, DHEAS: 100 uM) in OAT-K1-expressing MDCK cells2001The Journal of pharmacology and experimental therapeutics, Oct, Volume: 299, Issue:1
Multispecific substrate recognition of kidney-specific organic anion transporters OAT-K1 and OAT-K2.
AID681135TP_TRANSPORTER: uptake in OATP-F-expressing CHO cells2002Molecular endocrinology (Baltimore, Md.), Oct, Volume: 16, Issue:10
Identification of a novel human organic anion transporting polypeptide as a high affinity thyroxine transporter.
AID681877TP_TRANSPORTER: uptake in membrane vesicles from MRP4-expressing Sf9 cells2004The international journal of biochemistry & cell biology, Feb, Volume: 36, Issue:2
Multidrug resistance protein 4 (MRP4/ABCC4) mediates efflux of bimane-glutathione.
AID681150TP_TRANSPORTER: uptake in Xenopus laevis oocytes2001Pflugers Archiv : European journal of physiology, Nov, Volume: 443, Issue:2
Localization of organic anion transporting polypeptide 4 (Oatp4) in rat liver and comparison of its substrate specificity with Oatp1, Oatp2 and Oatp3.
AID679475TP_TRANSPORTER: uptake in Xenopus laevis oocytes2001Gastroenterology, Feb, Volume: 120, Issue:2
Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver.
AID324924Agonist activity at human TGR5 expressed in CHO cells by luciferase assay relative to lithocholic acid2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.
AID678960TP_TRANSPORTER: uptake in OATP-C-expressing 293c18 cells1999The Journal of biological chemistry, Dec-24, Volume: 274, Issue:52
A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters.
AID681577TP_TRANSPORTER: uptake in OAT-K2-expressing MDCK cells2001The Journal of pharmacology and experimental therapeutics, Oct, Volume: 299, Issue:1
Multispecific substrate recognition of kidney-specific organic anion transporters OAT-K1 and OAT-K2.
AID681899TP_TRANSPORTER: inhibition of Taurocholate uptake in the presence of Dehydroepiandrosterone-3-sulfate at a concentration of 5uM in membrane vesicles from MRP4-expressing V79 cells2003Hepatology (Baltimore, Md.), Aug, Volume: 38, Issue:2
Cotransport of reduced glutathione with bile salts by MRP4 (ABCC4) localized to the basolateral hepatocyte membrane.
AID205786Michaelis-Menten constant was determined in HEK293 cells2000Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
Structure-activity relationships of 17alpha-derivatives of estradiol as inhibitors of steroid sulfatase.
AID680197TP_TRANSPORTER: inhibition of E1S uptake (E1S: 0.05 uM, DHEAS: 500 uM) in Xenopus laevis oocytes2000The Journal of biological chemistry, Feb-11, Volume: 275, Issue:6
Molecular cloning and characterization of multispecific organic anion transporter 4 expressed in the placenta.
AID588967Substrates of transporters of clinical importance in the absorption and disposition of drugs, OATP1A22010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID681226TP_TRANSPORTER: inhibition of E1S uptake (E1S: 0.05 uM, DHEAS: 5 uM) in Xenopus laevis oocytes2001Molecular pharmacology, May, Volume: 59, Issue:5
Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney.
AID678971TP_TRANSPORTER: uptake in Xenopus laevis oocytes2000The Journal of biological chemistry, Feb-11, Volume: 275, Issue:6
Molecular cloning and characterization of multispecific organic anion transporter 4 expressed in the placenta.
AID678809TP_TRANSPORTER: uptake in Xenopus laevis oocytes2001Gastroenterology, Jun, Volume: 120, Issue:7
LST-2, a human liver-specific organic anion transporter, determines methotrexate sensitivity in gastrointestinal cancers.
AID679643TP_TRANSPORTER: uptake in Xenopus laevis oocytes2001Biochimica et biophysica acta, Mar-19, Volume: 1518, Issue:1-2
Functional analysis and androgen-regulated expression of mouse organic anion transporting polypeptide 1 (Oatp1) in the kidney.
AID681342TP_TRANSPORTER: uptake in Xenopus laevis oocytes1999The Journal of biological chemistry, Jun-11, Volume: 274, Issue:24
Identification of a novel gene family encoding human liver-specific organic anion transporter LST-1.
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID680995TP_TRANSPORTER: inhibition of E1S uptake by Dehydroepiandrosterone-3-sulfate at a concentration of 30uM in membrane vesicle from BCRP-expressing K562 cells2003Molecular pharmacology, Sep, Volume: 64, Issue:3
Breast cancer resistance protein exports sulfated estrogens but not free estrogens.
AID681149TP_TRANSPORTER: uptake in Xenopus laevis oocytes2001Pflugers Archiv : European journal of physiology, Nov, Volume: 443, Issue:2
Localization of organic anion transporting polypeptide 4 (Oatp4) in rat liver and comparison of its substrate specificity with Oatp1, Oatp2 and Oatp3.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (3,926)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990627 (15.97)18.7374
1990's965 (24.58)18.2507
2000's1293 (32.93)29.6817
2010's868 (22.11)24.3611
2020's173 (4.41)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 105.57

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index105.57 (24.57)
Research Supply Index8.42 (2.92)
Research Growth Index4.61 (4.65)
Search Engine Demand Index197.92 (26.88)
Search Engine Supply Index2.01 (0.95)

This Compound (105.57)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials412 (9.98%)5.53%
Reviews279 (6.76%)6.00%
Case Studies119 (2.88%)4.05%
Observational23 (0.56%)0.25%
Other3,294 (79.82%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]