Details of the Target

General Information of Target

Target ID LDTP03835
Target Name 17-beta-hydroxysteroid dehydrogenase type 2 (HSD17B2)
Gene Name HSD17B2
Gene ID 3294
Synonyms
EDH17B2; SDR9C2; 17-beta-hydroxysteroid dehydrogenase type 2; 17-beta-HSD 2; 20 alpha-hydroxysteroid dehydrogenase; 20-alpha-HSD; E2DH; Estradiol 17-beta-dehydrogenase 2; EC 1.1.1.62; Microsomal 17-beta-hydroxysteroid dehydrogenase; Short chain dehydrogenase/reductase family 9C member 2; Testosterone 17-beta-dehydrogenase; EC 1.1.1.239
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSTFFSDTAWICLAVPTVLCGTVFCKYKKSSGQLWSWMVCLAGLCAVCLLILSPFWGLIL
FSVSCFLMYTYLSGQELLPVDQKAVLVTGGDCGLGHALCKYLDELGFTVFAGVLNENGPG
AEELRRTCSPRLSVLQMDITKPVQIKDAYSKVAAMLQDRGLWAVINNAGVLGFPTDGELL
LMTDYKQCMAVNFFGTVEVTKTFLPLLRKSKGRLVNVSSMGGGAPMERLASYGSSKAAVT
MFSSVMRLELSKWGIKVASIQPGGFLTNIAGTSDKWEKLEKDILDHLPAEVQEDYGQDYI
LAQRNFLLLINSLASKDFSPVLRDIQHAILAKSPFAYYTPGKGAYLWICLAHYLPIGIYD
YFAKRHFGQDKPMPRALRMPNYKKKAT
Target Bioclass
Enzyme
Family
Short-chain dehydrogenases/reductases (SDR) family
Subcellular location
Endoplasmic reticulum membrane
Function
Catalyzes the NAD-dependent oxidation of the highly active 17beta-hydroxysteroids, such as estradiol (E2), testosterone (T), and dihydrotestosterone (DHT), to their less active forms and thus regulates the biological potency of these steroids. Oxidizes estradiol to estrone, testosterone to androstenedione, and dihydrotestosterone to 5alpha-androstan-3,17-dione. Also has 20-alpha-HSD activity.
Uniprot ID
P37059
Ensemble ID
ENST00000199936.9
HGNC ID
HGNC:5211
ChEMBL ID
CHEMBL2789

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
YN-4
 Probe Info  		100.00  LDD0445  [1]
IPM
 Probe Info  		N.A.  LDD0241  [2]
DBIA
 Probe Info  		C99(1.29); C188(1.48)  LDD3368  [3]
Acrolein
 Probe Info  		N.A.  LDD0224  [4]
W1
 Probe Info  		N.A.  LDD0236  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 A2780 C188(1.27)  LDD2254  [3]
 LDCM0023  KB03 BRX82 C188(1.97)  LDD2695  [3]
 LDCM0024  KB05 OAW-28 C99(1.29); C188(1.48)  LDD3368  [3]
 LDCM0109  NEM HeLa N.A.  LDD0224  [4]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Estradiol Acetate Small molecular drug DB13952
Estradiol Cypionate Small molecular drug DB13954
Estradiol Valerate Small molecular drug DB13956
Nadh Small molecular drug DB00157
Estradiol Benzoate . DB13953
Estradiol Dienanthate . DB13955

References

1 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
2 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
3 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
4 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.