title: Type 2 17-β hydroxysteroid dehydrogenase as a novel target for the treatment of osteoporosis.
abstract: Low estradiol level in postmenopausal women is implicated in osteoporosis, which occurs because of the high bone resorption rate. Estrogen formation is controlled by 17-β hydroxysteroid dehydrogenase 17-β HSD enzymes, where 17-β HSD type 1 contributes in the formation of estradiol, while type 2 catalyzes its catabolism. Inhibiting 17-β HSD2 can help in increasing estradiol concentration. Several promising 17-β HSD2 inhibitors that can act at low nanomolar range have been identified. However, there are some specific challenges associated with the application of these compounds. Our review provides an up-to-date summary of the current status and recent progress in the production of 17-β HSD2 inhibitors as well as the future challenges in their clinical application.
authors.affiliation: Laboratoire de Chimie Pharmaceutique Organique, Faculté de Pharmacie, Université Libre de Bruxelles, Campusplaine, CP 205/5, 1050 Brussels, Belgium.
authors.forename: Jalal
authors.initials: J
authors.lastname: Soubhye
authors.affiliation: Laboratoire de Pharmacie Galénique et Biopharmacie, Faculté de Pharmacie, Université Libre de Bruxelles, Brussels, Belgium.
authors.forename: Ibaa Chikh
authors.initials: IC
authors.lastname: Alard
authors.affiliation: Laboratoire de Chimie Pharmaceutique Organique, Faculté de Pharmacie, Université Libre de Bruxelles, Campusplaine, CP 205/5, 1050 Brussels, Belgium.|Analytical Platform of the Faculty of Pharmacy, Université Libre de Bruxelles, Brussels, Belgium.
authors.forename: Pierre
authors.initials: P
authors.lastname: van Antwerpen
authors.affiliation: Laboratoire de Chimie Pharmaceutique Organique, Faculté de Pharmacie, Université Libre de Bruxelles, Campusplaine, CP 205/5, 1050 Brussels, Belgium.
authors.forename: François
authors.initials: F
authors.lastname: Dufrasne
mesh_terms: D000818:Animals; D055808:Drug Discovery / Q000379:methods; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D004960:Estradiol Dehydrogenases / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism*; D006801:Humans; D008958:Models, Molecular; D010024:Osteoporosis / Q000188:drug therapy* / Q000201:enzymology* / Q000473:pathology
chemical_list: D004791:Enzyme Inhibitors; D004960:Estradiol Dehydrogenases; C523763:HSD17B2 protein, human