אסיף מאגר המחקר החקלאי

Rationally designed neuropeptide antagonists: A novel approach for generation of environmentally friendly insecticides

Year:

1997

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Authors :

Volume :

3

Co-Authors:

Gilon, C., Department of Organic Chemistry, Institute of Chemistry, Hebrew University of Jerusalem, Jerusalem 91904, Israel
Zeltser, I., Department of Organic Chemistry, Institute of Chemistry, Hebrew University of Jerusalem, Jerusalem 91904, Israel
Daniel, S., Department of Entomology, Volcani Center for Agricultural Research, Bet Dagan 50250, Israel
Ben-Aziz, O., Department of Entomology, Volcani Center for Agricultural Research, Bet Dagan 50250, Israel
Schefler, I., Department of Entomology, Volcani Center for Agricultural Research, Bet Dagan 50250, Israel
Altstein, M., Department of Entomology, Volcani Center for Agricultural Research, Bet Dagan 50250, Israel

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Abstract:

We report our approach for the generation of a novel type of putative insecticides based on backbone cyclic peptidomimetic antagonists of insect neuropeptides using pheromone biosynthesis activating neuropeptide (PBAN) as a model. This approach, called the backbone cyclic neuropeptide based antagonist (BBC-NBA), includes the following steps: (i) elucidation of the active sequence of the chosen insect neuropeptide; (ii) disclosure of a lead antagonist based on the sequence found in step (i); (iii) design and synthesis of backbone cyclic peptide libraries (cycloscan) based on the sequence of the lead antagonist; and (iv) design and synthesis of a peptidomimetic prototype insecticide. The BBC-NBA approach was applied to PBAN and led to the discovery of a potent linear lead antagonist and a potent backbone cyclic antagonist devoid of agonistic activity which inhibited sex pheromone biosynthesis in Heliothis peltigera female moths.

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