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    cis-peptide bond mimetic tetrazole analogs of the insect kinins identify the active conformation

    Nachman, R.J. and Zabrocki, J. and Olczak, J. and Williams, H.J. and Moyna, G. and Ian Scott, A. and Coast, Geoffrey (2002) cis-peptide bond mimetic tetrazole analogs of the insect kinins identify the active conformation. Peptides 23 (4), pp. 709-716. ISSN 0196-9781.

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    Abstract

    The insect kinin neuropeptides have been implicated in the regulation of water balance, digestive organ contraction, and energy mobilization in a number of insect species. A previous solution conformation study of an active, restricted-conformation cyclic analog, identified two possible turn conformations as the likely active conformation adopted by the insect kinins at the receptor site. These were a cisPro type VI β-turn over C-terminal pentapeptide core residues 1–4 and a transPro type I-like β-turn over core residues 2–5, present in a ratio of 60:40. Synthesis and evaluation of the diuretic activity of insect kinin analogs incorporating a tetrazole moiety, which mimics a cis peptide bond, identifies the active conformation as the former. The discovery of a receptor interaction model can lead to the development of potent agonist and antagonist analogs of the insect kinins. Indeed, in this study a tetrazole analog with D stereochemistry has been shown to demonstrate partial antagonism of the diuretic activity of natural insect kinins, providing a lead for more potent and effective antagonists of this critical neuropeptide family. The future development of mimetic agonists and antagonists of insect kinin neuropeptides will provide important tools to neuroendocrinologists studying the mechanisms by which they operate and to researchers developing new, environmentally friendly pest insect control strategies.

    Metadata

    Item Type: Article
    School: Birkbeck Schools and Departments > School of Science > Biological Sciences
    Depositing User: Sarah Hall
    Date Deposited: 20 May 2019 12:18
    Last Modified: 20 May 2019 12:18
    URI: http://eprints.bbk.ac.uk/id/eprint/27577

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