Target Information
Target General Infomation | |||||
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Target ID |
T44011
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Former ID |
TTDR00587
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Target Name |
Estradiol 17 beta-dehydrogenase 1
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Gene Name |
HSD17B1
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Synonyms |
17-beta-HSD 1; 17-beta-Hydroxysteroid dehydrogenase type 1; 20 alpha-hydroxysteroid dehydrogenase; 20-alpha-HSD; E2DH; Placental 17-beta-hydroxysteroid dehydrogenase; HSD17B1
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Target Type |
Clinical Trial
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Function |
Favors the reduction of estrogens and androgens. Also has 20-alpha-HSD activity. Uses preferentially NADH.
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BioChemical Class |
Short-chain dehydrogenases reductases
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Target Validation |
T44011
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UniProt ID | |||||
EC Number |
EC 1.1.1.62
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Sequence |
MARTVVLITGCSSGIGLHLAVRLASDPSQSFKVYATLRDLKTQGRLWEAARALACPPGSL
ETLQLDVRDSKSVAAARERVTEGRVDVLVCNAGLGLLGPLEALGEDAVASVLDVNVVGTV RMLQAFLPDMKRRGSGRVLVTGSVGGLMGLPFNDVYCASKFALEGLCESLAVLLLPFGVH LSLIECGPVHTAFMEKVLGSPEEVLDRTDIHTFHRFYQYLAHSKQVFREAAQNPEEVAEV FLTALRAPKPTLRYFTTERFLPLLRMRLDDPSGSNYVTAMHREVFGDVPAKAEAGAEAGG GAGPGAEDEAGRGAVGDPELGDPPAAPQ |
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Structure |
1A27; 1BHS; 1DHT; 1EQU; 1FDS; 1FDT; 1FDU; 1FDV; 1FDW; 1I5R; 1IOL; 1JTV; 1QYV; 1QYW; 1QYX; 3DEY; 3DHE; 3HB4; 3HB5; 3KLM; 3KLP; 3KM0
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Drugs and Mode of Action | |||||
Inhibitor | 1,1':4',1''-terphenyl-3,3''-diol | Drug Info | [530450] | ||
1,1':4',1''-terphenyl-3,4''-diol | Drug Info | [530450] | |||
1-Bromo-6-(3-hydroxyphenyl)-2-naphthol | Drug Info | [529595] | |||
16-(2',2'-Dimethyl)-propylidene-estradiol | Drug Info | [528033] | |||
16-(2',2'-Dimethyl)-propylidene-estrone | Drug Info | [528033] | |||
16-(4-cyano-benzylidene)-estradiol | Drug Info | [528033] | |||
16-(4-dimethylamino-benzylidene)-estradiol | Drug Info | [528033] | |||
16-(4-dimethylamino-benzylidene)-estrone | Drug Info | [528033] | |||
16-(pyridin-2-yl)methyl-estradiol | Drug Info | [528033] | |||
16-(pyridin-2-yl)methylene-estradiol | Drug Info | [528033] | |||
16-(pyridin-3-yl)methyl-estradiol | Drug Info | [528033] | |||
16-(pyridin-3-yl)methylene-estradiol | Drug Info | [528033] | |||
16-(pyridin-4-yl)methyl-estradiol | Drug Info | [528033] | |||
16-(pyridin-4-yl)methylene-estradiol | Drug Info | [528033] | |||
16-(thiophen-2-yl)methylene-estrone | Drug Info | [528033] | |||
16-beta-ethoxymethyl-estrone | Drug Info | [528033] | |||
16-beta-hydroxymethyl-estradiol | Drug Info | [528033] | |||
16-isobutylidene-estradiol | Drug Info | [528033] | |||
16-isobutylidene-estrone | Drug Info | [528033] | |||
16beta-cyano-estradiol | Drug Info | [528033] | |||
2'-Monophosphoadenosine 5'-Diphosphoribose | Drug Info | [551393] | |||
2-(3-hydroxyphenyl)quinolin-6-ol | Drug Info | [529359] | |||
2-Fluoro-4-[5-(3-hydroxyphenyl)-2-thienyl]phenol | Drug Info | [530450] | |||
2-Fluoro-4-[5-(3-hydroxyphenyl)-3-thienyl]phenol | Drug Info | [530450] | |||
2-Fluoro-5-[5-(4-hydroxyphenyl)-2-thienyl]phenol | Drug Info | [530450] | |||
2-Hydroxy-N,6-bis(3-hydroxyphenyl)-1-naphthamide | Drug Info | [529595] | |||
3'-(1-Benzothien-2-yl)biphenyl-3-ol | Drug Info | [530868] | |||
3'-(5-Chloro-2-thienyl)biphenyl-3-ol | Drug Info | [530868] | |||
3,3',3''-Thiene-2,3,5-triyltriphenol | Drug Info | [530450] | |||
3,3'-(1,2,4,5-tetrazine-3,6-diyl)diphenol | Drug Info | [529748] | |||
3,3'-(1,2,4-Thiadiazol-2,5-diyl)diphenol | Drug Info | [529748] | |||
3,3'-(1,2,4-thiadiazole-3,5-diyl)diphenol | Drug Info | [529748] | |||
3,3'-(1,3-Thiazol-2,4-diyl)diphenol | Drug Info | [529748] | |||
3,3'-(3-Methylthiene-2,5-diyl]diphenol | Drug Info | [530450] | |||
3,3'-(3-Phenylthiene-2,5-diyl)diphenol | Drug Info | [530450] | |||
3,3'-pyrazine-2,5-diyldiphenol | Drug Info | [529748] | |||
3,3'-Pyridine-2,5-diyldiphenol | Drug Info | [529748] | |||
3,3'-Thiene-2,4-diyldiphenol | Drug Info | [529748] | |||
3,3'-thiene-2,5-diyldiphenol | Drug Info | [530450] | |||
3,3-(1,3-Thiazole-2,5-diyl)diphenol | Drug Info | [529748] | |||
3,4'-(thiophene-2,4-diyl)diphenol | Drug Info | [530450] | |||
3-(2-naphthyl)phenol | Drug Info | [529359] | |||
3-(3-hydroxyphenyl)quinolin-7-ol | Drug Info | [529359] | |||
3-(5-phenyl-2-thienyl)phenol | Drug Info | [530450] | |||
3-(6-hydroxy-2-naphthyl)benzoic acid | Drug Info | [529359] | |||
3-Beta-Hydroxy-5-Androsten-17-One | Drug Info | [551393] | |||
3-Fluoro-5-[5-(4-hydroxyphenyl)-2-thienyl]phenol | Drug Info | [530450] | |||
3-Hydroxy-7-(3-hydroxyphenyl)-1-naphthonitrile | Drug Info | [529595] | |||
3-[2-(5-Chloro-2-thienyl)pyridin-4-yl]phenol | Drug Info | [530868] | |||
3-[3-(4-hydroxyphenyl)isoxazol-5-yl]phenol | Drug Info | [529504] | |||
3-[4-(4-Hydroxyphenyl)-1,3-oxazol-2-yl]phenol | Drug Info | [529504] | |||
3-[4-(5-Chloro-2-thienyl)pyridin-2-yl]phenol | Drug Info | [530868] | |||
3-[5-(3,4-Difluorophenyl)-2-thienyl]phenol | Drug Info | [530450] | |||
3-[5-(3-Fluorophenyl)-2-thienyl]phenol | Drug Info | [530450] | |||
3-[5-(4-Fluorophenyl)-2-thienyl]phenol | Drug Info | [530450] | |||
3-[5-(4-hydroxyphenyl)-1,3-oxazol-2-yl]phenol | Drug Info | [529748] | |||
3-[5-(4-hydroxyphenyl)-1,3-thiazol-2-yl]phenol | Drug Info | [530450] | |||
3-[5-(4-Hydroxyphenyl)-2-thienyl]-5-methylphenol | Drug Info | [530450] | |||
3-[5-(4-hydroxyphenyl)-2-thienyl]phenol | Drug Info | [530450] | |||
3-[5-(4-Hydroxyphenyl)-3-thienyl]phenol | Drug Info | [529748] | |||
3-[6-(5-Chloro-2-thienyl)pyridin-2-yl]phenol | Drug Info | [530868] | |||
4'-(5-Chloro-2-thienyl)biphenyl-3-ol | Drug Info | [530868] | |||
4'-(6-Methoxypyridin-3-yl)biphenyl-3-ol | Drug Info | [530868] | |||
4-ANDROSTENE-3-17-DIONE | Drug Info | [551374] | |||
4-Fluoro-1,1':4',1''-terphenyl-3,3''-diol | Drug Info | [530450] | |||
4-Methyl-1,1':4',1''-terphenyl-3,4''-diol | Drug Info | [530450] | |||
4-[5-(3-Hydroxyphenyl)-2-thienyl)-2-methyl]phenol | Drug Info | [530450] | |||
4-[5-(3-Hydroxyphenyl)-2-thienyl]benzene-1,2-diol | Drug Info | [530450] | |||
4-[5-(3-Hydroxyphenyl)-3-thienyl]-2-methylphenol | Drug Info | [530450] | |||
5-(6-hydroxy-2-naphthyl)pyridin-3-ol | Drug Info | [529359] | |||
5alpha-Androstan-3,17-Dione | Drug Info | [551393] | |||
6-(3-Hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [529595] | |||
6-(3-Hydroxyphenyl)-1-phenyl-2-naphthol | Drug Info | [529595] | |||
6-(4-Hydroxy-phenyl)-naphthalen-1-ol | Drug Info | [529359] | |||
6-oxo-16-formyl-estrone | Drug Info | [528033] | |||
6-oxo-estrone | Drug Info | [528033] | |||
7-(3-Hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [529359] | |||
7-Hydroxy-3-(3-hydroxyphenyl)-1-naphthonitrile | Drug Info | [529595] | |||
APIGENIN | Drug Info | [529519] | |||
EM-1745 | Drug Info | [551393] | |||
Equilin | Drug Info | [551393] | |||
Ethyl estrone-16-methylcarboxylate | Drug Info | [528033] | |||
KAEMPFEROL | Drug Info | [529519] | |||
Methyl estradiol-16-beta-carboxylate | Drug Info | [528033] | |||
N,N-diethyl estrone-16-methyl carboxamide | Drug Info | [528033] | |||
N-(1'-Phenyl-ethyl) estradiol-16-carboxamide | Drug Info | [528033] | |||
N-(4'-methyl-piperazinyl) estradiol-16-carboxamide | Drug Info | [528033] | |||
N-(furan-2-ylmethyl)-estrone-16-methyl carboxamide | Drug Info | [528033] | |||
N-(furan-2-ylmethyl)estradiol-16-carboxamide | Drug Info | [528033] | |||
N-(pyridin-3-ylmethyl) estradiol-16-carboxamide | Drug Info | [528033] | |||
N-(pyridin-4-ylmethyl) estradiol-16-carboxamide | Drug Info | [528033] | |||
N-ethyl estradiol-16-methyl carboxamide | Drug Info | [528033] | |||
N-ethyl estrone-16-methyl carboxamide | Drug Info | [528033] | |||
N-isopropyl estradiol-16-carboxamide | Drug Info | [528033] | |||
N-isopropyl estradiol-16-methyl carboxamide | Drug Info | [528033] | |||
N-isopropyl estrone-16-methyl carboxamide | Drug Info | [528033] | |||
N-methoxyethyl estrone-16-methyl carboxamide | Drug Info | [528033] | |||
N-methyl estradiol-16-methyl carboxamide | Drug Info | [528033] | |||
N-methyl estrone-16-methyl carboxamide | Drug Info | [528033] | |||
N-methyl-N-ethyl estradiol-16-carboxamide | Drug Info | [528033] | |||
N-methyl-N-ethyl estrone-16-methyl carboxamide | Drug Info | [528033] | |||
N-N-diethyl estradiol-16-methyl carboxamide | Drug Info | [528033] | |||
NARINGENIN | Drug Info | [529519] | |||
Nicotinamide-Adenine-Dinucleotide | Drug Info | [551393] | |||
NSC-94258 | Drug Info | [529519] | |||
Agonist | 4-Androstenedione | Drug Info | [551393] | ||
Pathways | |||||
BioCyc Pathway | Superpathway of steroid hormone biosynthesis | ||||
Estradiol biosynthesis I | |||||
KEGG Pathway | Steroid hormone biosynthesis | ||||
Metabolic pathways | |||||
Ovarian steroidogenesis | |||||
NetPath Pathway | FSH Signaling Pathway | ||||
PANTHER Pathway | Androgen/estrogene/progesterone biosynthesis | ||||
PathWhiz Pathway | Androgen and Estrogen Metabolism | ||||
Reactome | The canonical retinoid cycle in rods (twilight vision) | ||||
WikiPathways | Steroid Biosynthesis | ||||
Metabolism of steroid hormones and vitamin D | |||||
Prostate Cancer | |||||
References | |||||
Ref 528033 | J Med Chem. 2006 Feb 23;49(4):1325-45.Modification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1. | ||||
Ref 529359 | J Med Chem. 2008 Apr 10;51(7):2158-69. Epub 2008 Mar 7.Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases. | ||||
Ref 529504 | Bioorg Med Chem. 2008 Jun 15;16(12):6423-35. Epub 2008 May 3.Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases. | ||||
Ref 529519 | J Med Chem. 2008 Jul 24;51(14):4188-99. Epub 2008 Jun 6.Discovery of nonsteroidal 17beta-hydroxysteroid dehydrogenase 1 inhibitors by pharmacophore-based screening of virtual compound libraries. | ||||
Ref 529595 | J Med Chem. 2008 Aug 14;51(15):4685-98. Epub 2008 Jul 17.Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. | ||||
Ref 529748 | J Med Chem. 2008 Nov 13;51(21):6725-39. Epub 2008 Oct 15.Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1). | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.New insights into the SAR and binding modes of bis(hydroxyphenyl)thiophenes and -benzenes: influence of additional substituents on 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitory activity and selectivity. |
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