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Insect neuropeptide antagonists
Author(s) -
Altstein Miriam
Publication year - 2001
Publication title -
peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.556
H-Index - 125
eISSN - 1097-0282
pISSN - 0006-3525
DOI - 10.1002/1097-0282(2001)60:6<460::aid-bip10181>3.0.co;2-y
Subject(s) - antagonist , neuropeptide , chemistry , insect , in vivo , pheromone , pharmacology , biochemistry , receptor , biology , microbiology and biotechnology , botany
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. © 2002 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 60: 460–473, 2001