Synthesis and biological activity of FGLamide allatostatin analogs with Phe(3) residue modifications
Synthesis and biological activity of FGLamide allatostatin analogs with Phe(3) residue modifications
复制标题
Phe(3) 残基修饰的 FGLamide 尿抑素类似物的合成和生物活性
DOI：
10.1002/psc.2906
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发表时间：
2016
影响因子：
2.1
通讯作者：
Tobe Stephen S.
中科院分区：
文献类型：
--
作者：
Xie Yong;Wang Meizi;Zhang Li;Wu Xiaoqing;Yang Xinling;Tobe Stephen S.
A FGLamide allatostatin neuropeptide mimic (H17) is a potential insect growth regulator which inhibits the production of juvenile hormone by the corpora allata. To find more evidence to reveal the structure–activity relationships of the Phe3residue in theC‐terminal conserved pentapeptide and search for novel analogs with high activity, a series of Phe3residue‐modified analogs were designed and synthesized usingH17as the lead compound. Bioassay using juvenile hormone (JH) production bycorpora allataof the cockroachDiploptera punctataindicated that analogs4,11, and13showed strong ability to inhibit JH productionin vitro, with IC50of 38.5, 22.5, and 26 nM, respectively. As well, the activity of analog2(IC50: 89.5 nM) proved roughly equivalent to that ofH17. Based on the primary structure–activity relationships of Phe3residue, we suggest that for analogs containing six‐membered aromatic rings, removing the methylene group of Phe3or ano‐halogen orp‐halogen‐substituted benzene ring could increase the ability to inhibit biosynthesis of JH. This study will be useful for the design of new allatostatin analogs for insect management. Copyright © 2016 European Peptide Society and John Wiley & Sons, Ltd.
