Co-Authors:
Altstein, M., Department of Entomology, Institute of Plant Protection, Volcani Center, Bet Dagan 50250, Israel
Ben-Aziz, O., Department of Entomology, Institute of Plant Protection, Volcani Center, Bet Dagan 50250, Israel
Schefler, I., Department of Entomology, Institute of Plant Protection, Volcani Center, Bet Dagan 50250, Israel
Zeltser, I., Institute of Chemistry, Hebrew University of Jerusalem, Jerusalem, Israel
Gilon, C., Institute of Chemistry, Hebrew University of Jerusalem, Jerusalem, Israel
Abstract:
The development of a new approach for the generation of a novel type of putative insect control agents based on backbone cyclic peptidomimetic antagonists of insect-neuropeptides is reported. The approach, termed the backbone cyclic neuropeptide based on antagonist (BBC-NBA) was applied to the insect pyrokinin/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 peptidomimetic antagonists, devoid of agonistic activity, which inhibited in vivo PBAN-mediated activities in moths. (C) 2000 Elsevier Science Ltd.