אסיף מאגר המחקר החקלאי

Backbone cyclic pheromone biosynthesis activating neuropeptide (PBAN) antagonists: Inhibition of melanization in the moth Spodoptera littoralis (Insecta, Lepidoptera)

Year:

2006

Source of publication :

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Volume :

27

Co-Authors:

Ben-Aziz, O., Department of Entomology, The Volcani Center, Bet Dagan, 50250, Israel
Zeltser, I., Department of Entomology, The Volcani Center, Bet Dagan, 50250, Israel
Bhargava, K., Department of Molecular Biology, Biochemistry School of Biological Sciences, University of Missouri, Kansas City, MO 64110, United States
Davidovitch, M., Department of Entomology, The Volcani Center, Bet Dagan, 50250, Israel
Altstein, M., Department of Entomology, The Volcani Center, Bet Dagan, 50250, Israel

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Abstract:

Antagonistic and agonistic activities of backbone cyclic (BBC) pheromone biosynthesis activating neuropeptide (PBAN) analogues were evaluated in an attempt to identify potent melanotropic antagonists, to gain an insight into their structure-activity relationship (SAR), and to discover molecules with selective and non-selective melanotropic and pheromonotropic properties. Eight potent melanotropic BBC antagonists and seven agonists were disclosed. SAR studies revealed that the structural requirements of the melanotropic and pheromonotropic agonists and antagonists are different. The cyclic structure of the BBC peptides was unimportant for antagonistic activity, and linearization retained their melanotropic and pheromonotropic antagonistic properties. Comparison of the antagonistic activities of the BBC and precyclic peptides with respect to both functions revealed eight selective antagonists (six that were selective melanotropic antagonists and two selective pheromonotropic antagonists) and four non-selective (melanotropic and pheromonotropic) antagonists. The selective melanotropic antagonists exhibited both, pure or mixed agonistic/antagonistic activities. The selective pheromonotropic compounds were pure antagonists. All non-selective compounds were pure antagonists. Comparison of the agonistic activities of the BBC peptides with respect to both functions revealed six selective melanotropic agonists and one non-selective agonistic compound. All compounds (whether selective or non-selective) exhibited pure agonistic activity. Discovery of the selective compounds hints at the possibility that the receptors that mediate the respective activities may have different properties. © 2006 Elsevier Inc. All rights reserved.

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