Nachman R J, Moyna G, Williams H J, Tobe S S, Scott A I
Veterinary Entomology Research Unit, FAPRL, Agricultural Research Service, USDA, College Station, TX 77845-2122, USA.
Bioorg Med Chem. 1998 Aug;6(8):1379-88. doi: 10.1016/s0968-0896(98)00129-1.
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.
咽侧体抑制素是昆虫合成的由6至18个氨基酸组成的肽，用于控制保幼激素的产生，而保幼激素反过来又调节包括变态和产卵在内的多种功能。通过固相肽合成方法制备了四种昆虫咽侧体抑制素神经肽类似物，这些类似物在负责生物活性的区域引入了促进转角形成的拟肽部分。生物测定表明，这些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，这四种类似物具有相似的构象，且在活性核心区域存在一个β转角。活性差异被认为是由于类似物非天然部分原子的体积和相对位置不同，以及它们不同程度的构象自由度所致。这些研究支持了开发抗肽酶失活的基于神经肽的昆虫控制剂的可行性。
