Insect neuropeptide antagonists.
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.
Altstein
M
M
Institute of Plant Protection, the Volcani Center, Bet Dagan, Israel. vinnie2@agri.gov.il
D000595:Amino Acid Sequence; D000818:Animals; D007301:Insect Hormones / Q000037:antagonists & inhibitors / Q000737:chemistry*; D008969:Molecular Sequence Data; D009479:Neuropeptides / Q000037:antagonists & inhibitors / Q000737:chemistry*; D011487:Protein Conformation
D007301:Insect Hormones; D009479:Neuropeptides