Synthesis, biological activity, and conformational studies of insect allatostatin neuropeptide analogues incorporating turn-promoting moieties
Synthesis, biological activity, and conformational studies of insect allatostatin neuropeptide analogues incorporating turn-promoting moieties
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DOI：
10.1016/s0968-0896(98)00129-1
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发表时间：
1998-08-01
影响因子：
3.5
通讯作者：
Scott, AI
中科院分区：
文献类型：
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作者：
Nachman, RJ;Moyna, G;Scott, AI
Allatostins是昆虫合成的6-18个氨基酸多肽，用于控制保幼激素的产生，保幼激素反过来调节包括变态和产卵在内的功能。采用固相法合成了4种昆虫促转位假肽类似物，并在该区域具有一定的生物活性。生物活性测定表明，四个类似物的活性接近天然神经肽，基于核磁共振数据的分子模型显示，四个类似物的活性核心区存在类似的构象和β-转折。活性的差异被认为是由于类似物非自然部分原子的体积和相对位置的不同，以及它们不同的构象自由度所致。这些研究支持了开发抗肽酶失活的神经肽类杀虫剂的可行性。(C)1998由爱思唯尔科学有限公司出版。版权所有。
Allatostatins are 6-18 amino acid peptides synthezed by insects to control production of juvenile hormones, which in turn regulate functions including metamorphosis and egg production. Four insect allatostatin neuropeptide analogues incorporating turn-promoting pseudopeptide moieties in the region responsible for biological activity were prepared by solid phase peptide synthetic methods. Bioassay indicated that activities approached those of the natural neuropeptides, and molecular models based on NMR data showed similar conformations and the presence of a beta-turn in the active core region for the four analogues. Differences in activity are believed to be due to differences in bulk and relative position of atoms in the unnatural portion of the analogues, and their differing degrees of conformational freedom. The studies support the feasibility of development of neuropeptide-based insect control agents resistant to peptidase deactivation. (C) 1998 Published by Elsevier Science Ltd. All rights reserved.