Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 10, Issue 6, Pages 985-990Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.9b00174
Keywords
Inhibitor; peptide; muscle atrophic disorder; myostatin; structure-activity relationship
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Funding
- Japan Society for the Promotion of Sciences (JSPS) KAKENHI [15H04658]
- MEXT [29-4]
- Grants-in-Aid for Scientific Research [15H04658] Funding Source: KAKEN
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Inhibition of myostatin is a promising strategy for treatment of muscle atrophic disorders. We had already identified a 23mer peptide (1) as a synthetic myostatin inhibitor, and structure activity relationship studies with 1 afforded a potent 22-mer peptide derivative (3). Herein, we report the shortest myostatin inhibitory peptide so far. Among chain-shortened 16-mer peptidic inhibitors derived from the C-terminal region of 3, peptide inhibitor 8a with beta-sheet propensity was twice as potent as 22-mer inhibitor 3 and significantly increased not only muscle mass but also hind limb grip strength in Duchenne muscular dystrophic model mice. These results suggest that 8a is a promising platform for drug development treating muscle atrophic disorders.
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