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hydroxysteroid 17-beta dehydrogenase 2

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Target not currently curated in GtoImmuPdb

Target id: 3094

Nomenclature: hydroxysteroid 17-beta dehydrogenase 2

Family: 1.-.-.- Oxidoreductases

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 387 16q23.3 HSD17B2 hydroxysteroid 17-beta dehydrogenase 2
Mouse 1 381 8 E1 Hsd17b2 hydroxysteroid (17-beta) dehydrogenase 2
Rat - 381 19q12 Hsd17b2 hydroxysteroid (17-beta) dehydrogenase 2
Previous and Unofficial Names Click here for help
17β-HSD2 | estradiol 17-beta-dehydrogenase 2 | HSD17 | SDR9C2 | short chain dehydrogenase/reductase family 9C, member 2
Database Links Click here for help
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Enzyme Reaction Click here for help
EC Number: 1.1.1.62 17β-estradiol + NAD+ = estrone + H+ + NADH
EC Number: 1.1.1.239

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 24 [PMID: 31343176] Small molecule or natural product Hs Inhibition 8.2 pIC50 1
pIC50 8.2 (IC50 6.1x10-9 M) [1]
compound 24 [PMID: 31343176] Small molecule or natural product Rn Inhibition 8.0 pIC50 1
pIC50 8.0 (IC50 1x10-8 M) [1]
compound 24 [PMID: 31343176] Small molecule or natural product Mm Inhibition 7.7 pIC50 1
pIC50 7.7 (IC50 2.2x10-8 M) [1]
View species-specific inhibitor tables
General Comments
17β-HSD2 catalyses the interconversion of estradiol <-> estrone and testosterone <-> androstenedione.
Pharmacological inhibition of 17β-HSD2 is being investigated as a novel mechanism for the treatment of osteoporosis. Inhibiting 17β-HSD2 is predicted to increase estradiol and testosterone levels in bone, and to thereby simultaneously inhibit osteoclast-mediated bone resorption and increase bone formation by osteoblasts.

References

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1. Abdelsamie AS, Salah M, Siebenbürger L, Merabet A, Scheuer C, Frotscher M, Müller ST, Zierau O, Vollmer G, Menger MD et al.. (2019) Design, Synthesis, and Biological Characterization of Orally Active 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors Targeting the Prevention of Osteoporosis. J Med Chem, 62 (15): 7289-7301. [PMID:31343176]

How to cite this page

1.-.-.- Oxidoreductases: hydroxysteroid 17-beta dehydrogenase 2. Last modified on 26/07/2019. Accessed on 08/05/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=3094.