par Soubhye, Jalal ;Chikh Alard, Ibaa ;Van Antwerpen, Pierre ;Dufrasne, François
Référence Future Medicinal Chemistry, 7, 11, page (1431-1456)
Publication Publié, 2015-08
Référence Future Medicinal Chemistry, 7, 11, page (1431-1456)
Publication Publié, 2015-08
Article révisé par les pairs
Résumé : | 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. |