Details of the Target

General Information of Target

Target ID LDTP02707
Target Name 3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1 (HSD3B1)
Gene Name HSD3B1
Gene ID 3283
Synonyms
3BH; HSDB3A; 3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1; 3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type I; 3-beta-HSD I; 3-beta-hydroxy-5-ene steroid dehydrogenase; 3-beta-hydroxy-Delta(5)-steroid dehydrogenase; EC 1.1.1.145; 3-beta-hydroxysteroid 3-dehydrogenase; EC 1.1.1.270; Delta-5-3-ketosteroid isomerase; Dihydrotestosterone oxidoreductase; EC 1.1.1.210; Steroid Delta-isomerase; EC 5.3.3.1; Trophoblast antigen FDO161G
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTGWSCLVTGAGGFLGQRIIRLLVKEKELKEIRVLDKAFGPELREEFSKLQNKTKLTVLE
GDILDEPFLKRACQDVSVIIHTACIIDVFGVTHRESIMNVNVKGTQLLLEACVQASVPVF
IYTSSIEVAGPNSYKEIIQNGHEEEPLENTWPAPYPHSKKLAEKAVLAANGWNLKNGGTL
YTCALRPMYIYGEGSRFLSASINEALNNNGILSSVGKFSTVNPVYVGNVAWAHILALRAL
QDPKKAPSIRGQFYYISDDTPHQSYDNLNYTLSKEFGLRLDSRWSFPLSLMYWIGFLLEI
VSFLLRPIYTYRPPFNRHIVTLSNSVFTFSYKKAQRDLAYKPLYSWEEAKQKTVEWVGSL
VDRHKETLKSKTQ
Target Bioclass
Enzyme
Family
3-beta-HSD family
Subcellular location
Endoplasmic reticulum membrane
Function
A bifunctional enzyme responsible for the oxidation and isomerization of 3beta-hydroxy-Delta(5)-steroid precursors to 3-oxo-Delta(4)-steroids, an essential step in steroid hormone biosynthesis. Specifically catalyzes the conversion of pregnenolone to progesterone, 17alpha-hydroxypregnenolone to 17alpha-hydroxyprogesterone, dehydroepiandrosterone (DHEA) to 4-androstenedione, and androstenediol to testosterone. Additionally, catalyzes the interconversion between 3beta-hydroxy and 3-oxo-5alpha-androstane steroids controlling the bioavalability of the active forms. Specifically converts dihydrotestosterone to its inactive form 5alpha-androstanediol, that does not bind androgen receptor/AR. Also converts androstanedione, a precursor of testosterone and estrone, to epiandrosterone. Expected to use NAD(+) as preferred electron donor for the 3beta-hydroxy-steroid dehydrogenase activity and NADPH for the 3-ketosteroid reductase activity (Probable).
Uniprot ID
P14060
Ensemble ID
ENST00000369413.8
HGNC ID
HGNC:5217
ChEMBL ID
CHEMBL1958

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C183(1.95)  LDD2282  [1]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STS-1
 Probe Info  		1.16  LDD0137  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 C-4-II C183(1.95)  LDD2282  [1]
 LDCM0023  KB03 C-4-II C183(3.44)  LDD2699  [1]
 LDCM0024  KB05 C-4-II C183(2.29)  LDD3116  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Dihydrolipoyllysine-residue succinyltransferase component of 2-oxoglutarate dehydrogenase complex, mitochondrial (DLST) 2-oxoacid dehydrogenase family P36957
Serine/threonine-protein kinase Nek7 (NEK7) NEK Ser/Thr protein kinase family Q8TDX7
Fibroblast growth factor receptor 3 (FGFR3) Tyr protein kinase family P22607
Transporter and channel
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Calreticulin (CALR) Calreticulin family P27797
Monocarboxylate transporter 13 (SLC16A13) Monocarboxylate porter (TC 2.A.1.13) family Q7RTY0
Aquaporin-6 (AQP6) MIP/aquaporin (TC 1.A.8) family Q13520
Transmembrane protein 14B (TMEM14B) TMEM14 family Q9NUH8
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Gelsolin (GSN) Villin/gelsolin family P06396

The Drug(s) Related To This Target

Approved
Click To Hide/Show 10 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Nadh Small molecular drug DB00157
Prasterone Small molecular drug DB01708
Tibolone Small molecular drug DB09070
Trilostane Small molecular drug DB01108
Hydrocortisone Acetate . DB14539
Hydrocortisone Butyrate . DB14540
Hydrocortisone Cypionate . DB14541
Hydrocortisone Phosphate . DB14542
Hydrocortisone Probutate . DB14543
Hydrocortisone Valerate . DB14544
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Hydrocortisone Aceponate . DB14538
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Androstenedione Small molecular drug DB01536

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 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.