Development of prohibitin ligands against osteoporosis.
Fiche publication
Date publication
octobre 2020
Journal
European journal of medicinal chemistry
Auteurs
Membres identifiés du Cancéropôle Est :
Dr DESAUBRY Laurent
Tous les auteurs :
Tabti R, Lamoureux F, Charrier C, Ory B, Heymann D, Bentouhami E, Désaubry L
Lien Pubmed
Résumé
Current therapeutic approaches to osteoporosis display some potential adverse effects and a limited efficacy on non-vertebral fracture reduction. Some sulfonylamidines targeting the scaffold proteins prohibitins-1 and 2 (PHB1/2) have been showed to inhibit the formation of osteoclasts in charge of bone resorption. Herein, we report the development of a second generation of anti-osteoclastic PHB ligands. The most potent compound, IN45, showed 88% inhibition at the low concentration of 5 μM, indicates that it might serve as a basis for the development of new antiosteoporotic drugs.
Mots clés
Osteoclastogenesis, Osteoporosis, Prohibitins, SAR, STAT3
Référence
Eur J Med Chem. 2020 Oct 23;:112961