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Li, Q-J. and Martinz-Green,M.

The pyrokinin (PK)/pheromone biosynthesis activating neuropeptide (PBAN) family of peptides is a multifunctional family that plays a major role in the physiology of insects. The presence of PK/PBAN peptides has been demonstrated in a variety of moths and in other non-lepidopteran species, and their mode of action has been studied extensively. Despite these studies, very little is known about the endogenous mechanism, and much remains to be determined concerning the structural, chemical and cellular basis of their activity. Most of these studies were performed with synthetic peptides and involved exogenous application (mainly by injection) of the tested compounds, which does not necessarily reflect the endogenous natural mechanisms. Currently, it is still not known which endogenous peptide(s) mediate(s) each of the in vivo functions, whether each function is mediated by a different peptide, and whether each peptide mediates one or several functions. It is also not clear whether these functions are mediated by the same receptor or by different receptors, or whether the receptors of the various PK/PBAN peptides share functional homologies. One way to obtain a better insight on the mode of activity of this family of peptides is by the characterization of their receptors. Currently very little is known on the receptors of the PK/PBAN family. Recently, we have developed a binding assay and characterized the properties of the PK/PBAN receptor using female moths (Heliothis peltigera) pheromone glands. A summary of our recent findings will be presented. A complementary approach for studying receptors is by means of receptor-selective agonists and antagonists. We have developed a novel approach, termed the backbone cyclic neuropeptide-based antagonist (BBC-NBA) for the discovery of neuropeptide antagonists. This approach has been applied to the insect PK/PBAN family and resulted in the discovery of highly potent, metabolically stable antagonists, devoid of agonistic activity. The application of the antagonists for the study of the functional diversity and characterization of the PK/PBAN receptors as well as their possible application as insect control agents will be discussed.

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Characterization of the pyrokinin/PBAN receptor [abstract]

Li, Q-J. and Martinz-Green,M.

The pyrokinin (PK)/pheromone biosynthesis activating neuropeptide (PBAN) family of peptides is a multifunctional family that plays a major role in the physiology of insects. The presence of PK/PBAN peptides has been demonstrated in a variety of moths and in other non-lepidopteran species, and their mode of action has been studied extensively. Despite these studies, very little is known about the endogenous mechanism, and much remains to be determined concerning the structural, chemical and cellular basis of their activity. Most of these studies were performed with synthetic peptides and involved exogenous application (mainly by injection) of the tested compounds, which does not necessarily reflect the endogenous natural mechanisms. Currently, it is still not known which endogenous peptide(s) mediate(s) each of the in vivo functions, whether each function is mediated by a different peptide, and whether each peptide mediates one or several functions. It is also not clear whether these functions are mediated by the same receptor or by different receptors, or whether the receptors of the various PK/PBAN peptides share functional homologies. One way to obtain a better insight on the mode of activity of this family of peptides is by the characterization of their receptors. Currently very little is known on the receptors of the PK/PBAN family. Recently, we have developed a binding assay and characterized the properties of the PK/PBAN receptor using female moths (Heliothis peltigera) pheromone glands. A summary of our recent findings will be presented. A complementary approach for studying receptors is by means of receptor-selective agonists and antagonists. We have developed a novel approach, termed the backbone cyclic neuropeptide-based antagonist (BBC-NBA) for the discovery of neuropeptide antagonists. This approach has been applied to the insect PK/PBAN family and resulted in the discovery of highly potent, metabolically stable antagonists, devoid of agonistic activity. The application of the antagonists for the study of the functional diversity and characterization of the PK/PBAN receptors as well as their possible application as insect control agents will be discussed.

Scientific Publication
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