Author
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Nachman, Ronald |
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Submitted to: Pacific Basin Society Chemical International Congress Abstracts
Publication Type: Abstract Only Publication Acceptance Date: 3/20/1995 Publication Date: N/A Citation: N/A Interpretive Summary: Technical Abstract: The importance of neuropeptides to the maintenance of critical physiological processes in insects has been established. Nevertheless, insect neuropeptides in and of themselves hold little promise as insect control agents because of their susceptibility to enzymatic degradation in the target insect, lability under environmental conditions, and inability to pass through the hydrophobic insect cuticle. The removal of the peptid nature (i.e. the constituent amide bonds) of insect neuropeptides represents a strategy that could overcome these limitations. Active non- peptide, peptidomimetic agonists and/or antagonists may hold promise for future utilization in pest insect control strategies. In this paper, we discuss enzymatic degradation by insect angiotensin-converting enzyme (ACE) of the insect kinin, insectatachykinin and pyrokinin neuropeptide families, and the synthesis of active analogs that are resistant to degradation. Conformationally-restricted analogs of the myosuppressin and insectatachykinin families shed light on the active conformation adopted at the receptor site. Utilization of this information for the development of peptidomimetic analogs is discussed. The first nonpeptide analog of an insect neuropeptide both mimics the biological activity and binds to a locust oviduct receptor site of the myosuppressin peptide family. |
