Details of the Target

General Information of Target

Target ID LDTP02708
Target Name 17-beta-hydroxysteroid dehydrogenase type 1 (HSD17B1)
Gene Name HSD17B1
Gene ID 3292
Synonyms
E17KSR; EDH17B1; EDH17B2; EDHB17; SDR28C1; 17-beta-hydroxysteroid dehydrogenase type 1; 17-beta-HSD 1; EC 1.1.1.51; 20 alpha-hydroxysteroid dehydrogenase; 20-alpha-HSD; E2DH; Estradiol 17-beta-dehydrogenase 1; EC 1.1.1.62; Placental 17-beta-hydroxysteroid dehydrogenase; Short chain dehydrogenase/reductase family 28C member 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MARTVVLITGCSSGIGLHLAVRLASDPSQSFKVYATLRDLKTQGRLWEAARALACPPGSL
ETLQLDVRDSKSVAAARERVTEGRVDVLVCNAGLGLLGPLEALGEDAVASVLDVNVVGTV
RMLQAFLPDMKRRGSGRVLVTGSVGGLMGLPFNDVYCASKFALEGLCESLAVLLLPFGVH
LSLIECGPVHTAFMEKVLGSPEEVLDRTDIHTFHRFYQYLAHSKQVFREAAQNPEEVAEV
FLTALRAPKPTLRYFTTERFLPLLRMRLDDPSGSNYVTAMHREVFGDVPAKAEAGAEAGG
GAGPGAEDEAGRGAVGDPELGDPPAAPQ
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Short-chain dehydrogenases/reductases (SDR) family
Subcellular location
Cytoplasm
Function Favors the reduction of estrogens and androgens. Converts estrone (E1) to a more potent estrogen, 17beta-estradiol (E2). Also has 20-alpha-HSD activity. Uses preferentially NADH.
TTD ID
T44011
Uniprot ID
P14061
DrugMap ID
TTIWB6L
Ensemble ID
ENST00000585807.6
HGNC ID
HGNC:5210
ChEMBL ID
CHEMBL3181

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C55(1.65); C157(3.68)  LDD2282  [1]
Sulforaphane-probe2
 Probe Info  		2.30  LDD0042  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 C-4-II C55(1.65); C157(3.68)  LDD2282  [1]
 LDCM0023  KB03 C-4-II C55(3.26); C157(9.00)  LDD2699  [1]
 LDCM0024  KB05 C-4-II C55(2.77); C157(5.67)  LDD3116  [1]
 LDCM0003  Sulforaphane MCF-7 2.30  LDD0042  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Polyunsaturated fatty acid 5-lipoxygenase (ALOX5) Lipoxygenase family P09917

The Drug(s) Related To This Target

Approved
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Nadh Small molecular drug DB00157
Prasterone Small molecular drug DB01708
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Naringenin Small molecular drug D02ABO
Investigative
Click To Hide/Show 105 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1,1':4',1''-terphenyl-3,3''-diol Small molecular drug D07JOZ
1,1':4',1''-terphenyl-3,4''-diol Small molecular drug D0C9KZ
1-bromo-6-(3-hydroxyphenyl)-2-naphthol Small molecular drug D08PDK
16-(2',2'-dimethyl)-propylidene-estradiol Small molecular drug D06ZNI
16-(2',2'-dimethyl)-propylidene-estrone Small molecular drug D0I0KV
16-(4-cyano-benzylidene)-estradiol Small molecular drug D0U7DJ
16-(4-dimethylamino-benzylidene)-estradiol Small molecular drug D0HR7O
16-(4-dimethylamino-benzylidene)-estrone Small molecular drug D02MQT
16-(Pyridin-2-yl)Methyl-estradiol Small molecular drug D0WM4K
16-(Pyridin-2-yl)Methylene-estradiol Small molecular drug D02XZO
16-(Pyridin-3-yl)Methyl-estradiol Small molecular drug D0N1LT
16-(Pyridin-3-yl)Methylene-estradiol Small molecular drug D08EHR
16-(Pyridin-4-yl)Methyl-estradiol Small molecular drug D06FPP
16-(Pyridin-4-yl)Methylene-estradiol Small molecular drug D01ERB
16-(Thiophen-2-yl)Methylene-estrone Small molecular drug D0A0CG
16-beta-ethoxymethyl-estrone Small molecular drug D0B9HX
16-beta-hydroxymethyl-estradiol Small molecular drug D0Z1AT
16-isobutylidene-estradiol Small molecular drug D0G4KT
16-isobutylidene-estrone Small molecular drug D01OCZ
16beta-cyano-estradiol Small molecular drug D0EK5U
2'-monophosphoadenosine 5'-diphosphoribose Small molecular drug D0J2FY
2-(3-hydroxyphenyl)Quinolin-6-ol Small molecular drug D0KG1D
2-fluoro-4-[5-(3-hydroxyphenyl)-2-thienyl]Phenol Small molecular drug D0M0KX
2-fluoro-4-[5-(3-hydroxyphenyl)-3-thienyl]Phenol Small molecular drug D0Q3AN
2-fluoro-5-[5-(4-hydroxyphenyl)-2-thienyl]Phenol Small molecular drug D03XHF
2-hydroxy-n,6-bis(3-hydroxyphenyl)-1-naphthamide Small molecular drug D02QLY
3'-(1-benzothien-2-yl)Biphenyl-3-ol Small molecular drug D00PUR
3'-(5-chloro-2-thienyl)Biphenyl-3-ol Small molecular drug D06CED
3,3',3''-thiene-2,3,5-triyltriphenol Small molecular drug D0Z1MJ
3,3'-(1,2,4,5-tetrazine-3,6-diyl)Diphenol Small molecular drug D0R3HP
3,3'-(1,2,4-thiadiazol-2,5-diyl)Diphenol Small molecular drug D0R5WV
3,3'-(1,2,4-thiadiazole-3,5-diyl)Diphenol Small molecular drug D0A4XA
3,3'-(1,3-thiazol-2,4-diyl)Diphenol Small molecular drug D0T6WL
3,3'-(3-methylthiene-2,5-diyl]Diphenol Small molecular drug D0P6JE
3,3'-(3-phenylthiene-2,5-diyl)Diphenol Small molecular drug D0B6SF
3,3'-pyrazine-2,5-diyldiphenol Small molecular drug D0DC3E
3,3'-pyridine-2,5-diyldiphenol Small molecular drug D07VXQ
3,3'-thiene-2,4-diyldiphenol Small molecular drug D08OQX
3,3'-thiene-2,5-diyldiphenol Small molecular drug D0TA0J
3,3-(1,3-thiazole-2,5-diyl)Diphenol Small molecular drug D00YNA
3,4'-(Thiophene-2,4-diyl)Diphenol Small molecular drug D0I5YT
3-(2-naphthyl)Phenol Small molecular drug D0F6ZH
3-(3-hydroxyphenyl)Quinolin-7-ol Small molecular drug D06NDT
3-(5-phenyl-2-thienyl)Phenol Small molecular drug D0G1DN
3-(6-hydroxy-2-naphthyl)Benzoic Acid Small molecular drug D0F0EI
3-fluoro-5-[5-(4-hydroxyphenyl)-2-thienyl]Phenol Small molecular drug D01JVG
3-hydroxy-7-(3-hydroxyphenyl)-1-naphthonitrile Small molecular drug D0D1KA
3-[2-(5-chloro-2-thienyl)Pyridin-4-yl]Phenol Small molecular drug D0QX5D
3-[3-(4-hydroxyphenyl)Isoxazol-5-yl]Phenol Small molecular drug D02UUR
3-[4-(4-hydroxyphenyl)-1,3-oxazol-2-yl]Phenol Small molecular drug D0IZ4Z
3-[4-(5-chloro-2-thienyl)Pyridin-2-yl]Phenol Small molecular drug D0A7PU
3-[5-(3,4-difluorophenyl)-2-thienyl]Phenol Small molecular drug D02BEJ
3-[5-(3-fluorophenyl)-2-thienyl]Phenol Small molecular drug D0A2GN
3-[5-(4-fluorophenyl)-2-thienyl]Phenol Small molecular drug D0UR6C
3-[5-(4-hydroxyphenyl)-1,3-oxazol-2-yl]Phenol Small molecular drug D0EL1Y
3-[5-(4-hydroxyphenyl)-1,3-thiazol-2-yl]Phenol Small molecular drug D00SLE
3-[5-(4-hydroxyphenyl)-2-thienyl]-5-methylphenol Small molecular drug D09GQE
3-[5-(4-hydroxyphenyl)-2-thienyl]Phenol Small molecular drug D01ZCG
3-[5-(4-hydroxyphenyl)-3-thienyl]Phenol Small molecular drug D0NM0P
3-[6-(5-chloro-2-thienyl)Pyridin-2-yl]Phenol Small molecular drug D05AIT
4'-(5-chloro-2-thienyl)Biphenyl-3-ol Small molecular drug D0Q6AD
4'-(6-methoxypyridin-3-yl)Biphenyl-3-ol Small molecular drug D0G5CP
4-androstene-3-17-dione Small molecular drug D0M8RO
4-fluoro-1,1':4',1''-terphenyl-3,3''-diol Small molecular drug D0BF3Y
4-methyl-1,1':4',1''-terphenyl-3,4''-diol Small molecular drug D0J8LU
4-[5-(3-hydroxyphenyl)-2-thienyl)-2-methyl]Phenol Small molecular drug D0Y2RL
4-[5-(3-hydroxyphenyl)-2-thienyl]Benzene-1,2-diol Small molecular drug D08OKP
4-[5-(3-hydroxyphenyl)-3-thienyl]-2-methylphenol Small molecular drug D01RZP
5-(6-hydroxy-2-naphthyl)Pyridin-3-ol Small molecular drug D0M3RQ
5alpha-androstan-3,17-dione Small molecular drug D0T5MO
6-(3-hydroxyphenyl)-1-phenyl-2-naphthol Small molecular drug D0V2QH
6-oxo-16-formyl-estrone Small molecular drug D02JRB
6-oxo-estrone Small molecular drug D03BZT
7-hydroxy-3-(3-hydroxyphenyl)-1-naphthonitrile Small molecular drug D04EPO
Apigenin Small molecular drug D00RIX
Em-1745 Small molecular drug D0W5CR
Equilin Small molecular drug D0R6DT
Ethyl Estrone-16-methylcarboxylate Small molecular drug D01AVM
Kaempferol Small molecular drug D0G3TK
Methyl Estradiol-16-beta-carboxylate Small molecular drug D0S2BW
N,N-diethyl Estrone-16-methyl Carboxamide Small molecular drug D0A5CD
N-(1'-phenyl-ethyl) Estradiol-16-carboxamide Small molecular drug D04CQM
N-(4'-methyl-piperazinyl) Estradiol-16-carboxamide Small molecular drug D08NFA
N-(Furan-2-ylmethyl)-estrone-16-methyl Carboxamide Small molecular drug D0K8VL
N-(Furan-2-ylmethyl)Estradiol-16-carboxamide Small molecular drug D0K6MM
N-(Pyridin-3-ylmethyl) Estradiol-16-carboxamide Small molecular drug D06AYL
N-(Pyridin-4-ylmethyl) Estradiol-16-carboxamide Small molecular drug D02DYZ
N-ethyl Estradiol-16-methyl Carboxamide Small molecular drug D0V5JV
N-ethyl Estrone-16-methyl Carboxamide Small molecular drug D0V4BE
N-isopropyl Estradiol-16-carboxamide Small molecular drug D08CXO
N-isopropyl Estradiol-16-methyl Carboxamide Small molecular drug D0B6SA
N-isopropyl Estrone-16-methyl Carboxamide Small molecular drug D0M4SL
N-methoxyethyl Estrone-16-methyl Carboxamide Small molecular drug D0Q9CI
N-methyl Estradiol-16-methyl Carboxamide Small molecular drug D0JI0Q
N-methyl Estrone-16-methyl Carboxamide Small molecular drug D01SGP
N-methyl-n-ethyl Estradiol-16-carboxamide Small molecular drug D0G7PB
N-n-diethyl Estradiol-16-methyl Carboxamide Small molecular drug D02MZN
Nicotinamide-adenine-dinucleotide Small molecular drug D0R6JE
Nsc-94258 Small molecular drug D01KKU
6-(3-hydroxy-phenyl)-naphthalen-2-ol . D0P8PK
6-(4-hydroxy-phenyl)-naphthalen-1-ol . D0H8PI
7-(3-hydroxy-phenyl)-naphthalen-2-ol . D01IAT
N-methyl-n-ethyl Estrone-16-methyl Carboxamide . D03XMR
Nicotinamide Adenine Dinucleotide Phosphate . DB03461
Stanolone Acetate . DB13951
Discontinued
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Androstanedione Small molecular drug DB01561
Androstenedione Small molecular drug DB01536
Stanolone Small molecular drug DB02901

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 Competition-based, quantitative chemical proteomics in breast cancer cells identifies new target profiles for sulforaphane. Chem Commun (Camb). 2017 May 4;53(37):5182-5185. doi: 10.1039/c6cc08797c.
Mass spectrometry data entry: PXD006279