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PubMed · 12209477

Insect neuropeptide antagonists.

M Altstein
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Abstract

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.

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Amino Acid SequenceAnimalsInsect HormonesMolecular Sequence DataNeuropeptidesProtein ConformationJournal ArticleResearch Support, Non-U.S. Gov'tReview

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M Altstein. 2001. Insect neuropeptide antagonists.. https://doi.org/10.1002/1097-0282(2001)60%3A6%3C460%3A%3Aaid-bip10181%3E3.0.co%3B2-y

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