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Interaction of Mimetic Analogs of Insect Kinin Neuropeptides with Arthropod Receptors

  • Ronald J. Nachman
  • Patricia V. Pietrantonio
Part of the Advances in Experimental Medicine and Biology book series (volume 692)

Abstract

Insect kinin neuropeptides share a common C-terminal pentapeptide sequence Phe1-Xaa1 2-Xaa2 3-Trp4-Gly5-NH2 (Xaa1 2?His, Asn, Phe, Ser or Tyr; Xaa2 3?Pro, Ser or Ala) and have been isolated from a number of insects, including species of Dictyoptera, Orthoptera and Lepidoptera. They have been associated with the regulation of such diverse processes as hindgut contraction, diuresis and the release of digestive enzymes. In this chapter, the chemical, conformational and stereochemical aspects of the activity of the insect kinins with expressed receptors and/or biological assays are reviewed. With this information, biostable analogs are designed that protect peptidase-susceptible sites in the insect kinin sequence and demonstrate significant retention of activity on both receptor and biological assays. The identification of the most critical residue of the insect kinins for receptor interaction is used to select a scaffold for a recombinant library that leads to identification of a nonpeptide mimetic analog. C-terminal aldehyde insect kinin analogs modify the activity of the insect kinins leading to inhibition of weight gain and mortality in corn earworm larvae and selective inhibition of diuresis in the housefly. Strategies for the modification of insect neuropeptide structures for the enhancement of the topical and oral bioavailability of insect neuropeptides and the promotion of time-release from the cuticle and/or foregut are reviewed. Promising mimetic analog leads for the development of selective agents capable of disrupting insect kinin regulated processes are identified that may provide interesting tools for arthropod endocrinologists and new pest insect management strategies in the future.

Keywords

Malpighian Tubule Kinin Receptor Pheromone Production Diuretic Activity Secretion Assay 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Landes Bioscience and Springer Science+Business Media 2010

Authors and Affiliations

  1. 1.Areawide Pest Management Research UnitSouthern Plains Agricultural Research Center, U.S. Department of AgricultureCollege StationUSA
  2. 2.Department of EntomologyTexas A&M UniversityCollege StationUSA

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