Development of Small-molecule Inhibitors Targeting Sclerostin Loop3 for Osteoporosis

Project: Research project

Project Details

Description

The monoclonal antibody romosozumab conferred high cardiovascular risk in clinical trials for the treatment of postmenopausal osteoporosis and brought compliance issues for patients who prefer oral therapy. Our in vitro and in vivo studies found that specifically targeting sclerostin loop 3 could promote bone formation without increasing cardiovascular risk, and hit compound YSF-1 targeting loop 3 was accordingly designed through virtual screening, structural modification, and in vitro binding experiments. Based on our previous studies, we will carry out artificial intelligence-guided de novo design and screening, organic synthesis and structure optimization, in vitro studies, 
pharmacodynamics, and pharmacokinetics, etc. to develop a new generation of oral 
small-molecule inhibitors targeting sclerostin loop 3 without increasing cardiovascular risk.
StatusFinished
Effective start/end date3/10/2326/01/25

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