European Journal of Medicinal Chemistry (2021)
Update date:2022-08-03
Topics: In vitro Testing Clinical Trials In Vivo Testing Combination Therapies Regulatory Approval Understanding the Role of Prohibitin in Osteoporosis Identification of Potential Ligands Design and Synthesis of Ligands Toxicology and Pharmacokinetics Market Launch and Post-Market Surveillance
Tabti, Redouane
Lamoureux, Fran?ois
Charrier, Céline
Ory, Benjamin
Heymann, Dominique
Bentouhami, Embarek
Désaubry, Laurent
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.
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