Development of prohibitin ligands against osteoporosis.

Authors :: Tabti R
Lamoureux F
Charrier C
Ory B
Heymann D
Bentouhami E
Désaubry L
Source :: European journal of medicinal chemistry [Eur J Med Chem] 2021 Jan 15; Vol. 210, pp. 112961. Date of Electronic Publication: 2020 Oct 23.
Publication Year :: 2021
Abstract: 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.<br />Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.<br /> (Copyright © 2020 Elsevier Masson SAS. All rights reserved.)