Altstein M
Institute of Plant Protection, the Volcani Center, Bet Dagan, Israel.
Biopolymers. 2001;60(6):460-73. doi: 10.1002/1097-0282(2001)60:6<460::AID-BIP10181>3.0.CO;2-Y.
The development of a new integrated approach to the generation of a novel type of insect neuropeptide (Np) antagonists and putative insect control agents based on backbone cyclic compounds is described. The approach, termed the backbone cyclic neuropeptide-based antagonist (BBC-NBA), was applied to the insect pyrokinin (PK)/pheromone biosynthesis activating neuropeptide (PBAN) family as a model, and led to the discovery of a potent linear lead antagonist and several highly potent, metabolically stable BBC antagonists, devoid of agonistic activity, which inhibited PBAN-mediated activities in moths in vivo. This review briefly summarizes our knowledge of insect Nps, describes the PK/PBAN Np family, presents the basic concepts behind the BBC-NBA approach, and introduces the advantages of this method for generation of Np agonists, antagonists and insecticide prototype molecules.
本文描述了一种新的综合方法的开发，该方法基于主链环状化合物生成新型昆虫神经肽（Np）拮抗剂和推定的昆虫控制剂。这种方法被称为基于主链环状神经肽的拮抗剂（BBC-NBA），以昆虫焦激肽（PK）/信息素生物合成激活神经肽（PBAN）家族为模型进行应用，并导致发现了一种有效的线性先导拮抗剂和几种高效、代谢稳定且无激动活性的BBC拮抗剂，这些拮抗剂在体内抑制了蛾类中PBAN介导的活性。本综述简要总结了我们对昆虫神经肽的了解，描述了PK/PBAN神经肽家族，介绍了BBC-NBA方法背后的基本概念，并介绍了该方法在生成Np激动剂、拮抗剂和杀虫剂原型分子方面的优势。
