Comprehensive analysis of a dipeptide library to identify ghrelin release-modulating peptides
Comprehensive analysis of a dipeptide library to identify ghrelin release-modulating peptides
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DOI：
10.1002/1873-3468.13522
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发表时间：
2019-07-12
期刊：
影响因子：
3.5
通讯作者：
Ohinata, Kousaku
中科院分区：
文献类型：
--
作者：
Nakato, Junya;Aoki, Hayato;Ohinata, Kousaku
我们进行了一个全面的分析生长激素释放肽释放调节活性的二肽库使用MGN 3 -1，生长激素释放肽生产细胞系。我们发现大多数二肽抑制ghrelin的分泌，而N-末端含Ser的二肽和少数其他二肽刺激它。N-末端氨基酸残基，而不是C-末端残基，在二肽的作用中起主导作用。在二肽中，Leu-Ile（LI）和Ser-Val（SV）分别最强烈地抑制和刺激ghrelin分泌。LI激活G（i）信号传导，SV通过MAPK途径起作用。口服给予的LI和SV分别降低和增加小鼠的血浆胃饥饿素水平和食物摄入。总之，LI和SV，发现基于一个二肽库的全面筛选，调节生长激素释放肽在体外和体内的分泌。
We performed a comprehensive analysis of ghrelin release-modulating activity of a dipeptide library using MGN3-1, a ghrelin-producing cell line. We found that most dipeptides suppress ghrelin secretion, whereas the N-terminal Ser-containing dipeptides and a few others stimulate it. N-terminal amino acid residues, but not C-terminal residues, play a dominant role in the effects of dipeptides. Among dipeptides, Leu-Ile (LI) and Ser-Val (SV) most strongly suppress and stimulate ghrelin secretion, respectively. LI activates G(i) signaling and SV acts via the MAPK pathway. Orally administered LI and SV reduce and increase plasma ghrelin levels and food intake in mice, respectively. In conclusion, LI and SV, found based on the comprehensive screening of a dipeptide library, modulate ghrelin secretion in vitro and in vivo.