Inhibition of myostatin is a promising strategy for treatment of muscle atrophic disorders. We had already identified a 23-mer peptide () as a synthetic myostatin inhibitor, and structure-activity relationship studies with afforded a potent 22-mer peptide derivative (). Herein, we report the shortest myostatin inhibitory peptide so far. Among chain-shortened 16-mer peptidic inhibitors derived from the C-terminal region of , peptide inhibitor with β-sheet propensity was twice as potent as 22-mer inhibitor and significantly increased not only muscle mass but also hind limb grip strength in Duchenne muscular dystrophic model mice. These results suggest that is a promising platform for drug development treating muscle atrophic disorders.
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6580550 | PMC |
http://dx.doi.org/10.1021/acsmedchemlett.9b00174 | DOI Listing |
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