Follistatin is well known as an inhibitor of transforming growth factor (TGF)-β superfamily ligands including myostatin and activin A. Myostatin, a negative regulator of muscle growth, is a promising target with which to treat muscle atrophic diseases. Here, we focused on the N-terminal domain (ND) of follistatin (Fst) that interacts with the type I receptor binding site of myostatin. Through bioassay of synthetic ND-derived fragment peptides, we identified DF-3, a new myostatin inhibitory 14-mer peptide which effectively inhibits myostatin, but fails to inhibit activin A or TGF-β1, in an in vitro luciferase reporter assay. Injected intramuscularly, DF-3 significantly increases skeletal muscle mass in mice and consequently, it can serve as a platform for development of muscle enhancement based on myostatin inhibition.

中文翻译：

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卵泡抑素衍生的肌生长抑制素抑制肽的发现。

卵泡抑素是众所周知的转化生长因子（TGF）-β超家族配体（包括肌生长抑制素和激活素A）的抑制剂。肌生长抑制素是肌肉生长的负调节剂，是治疗肌肉萎缩性疾病的有希望的靶标。在这里，我们专注于卵泡抑素（Fst）的N末端域（ND），该域与肌生长抑制素的I型受体结合位点相互作用。通过合成ND衍生片段肽的生物测定，我们在体外荧光素酶报告基因测定中鉴定了DF-3，DF-3是一种新型的抑制肌生长抑制素的14-mer肽，该肽可有效抑制肌生长抑制素，但不能抑制激活素A或TGF-β1。肌注DF-3可显着增加小鼠骨骼肌质量，因此，它可作为基于肌肉生长抑制素抑制作用的肌肉增强发展的平台。