An active insect kinin analog with 4-aminopyroglutamate, a novel cis-peptide bond, type VI beta-turn motif |
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Authors: | Nachman Ronald J Kaczmarek Krzysztof Williams Howard J Coast Geoffrey M Zabrocki Janusz |
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Institution: | Areawide Pest Management Research Unit, Southern Plains Agricultural Research Center, ARS, U.S. Department of Agriculture, 2881 F/B Rd., College Station, TX 77845, USA. nachman@tamu.edu |
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Abstract: | The insect kinins are potent diuretic peptides that preferentially form a cis-Pro, type VI beta-turn. An insect kinin analog containing (2S,4S)-4-aminopyroglutamate, a novel cis-peptide bond, type VI beta-turn motif, demonstrates significant activity in the physiological range in a cricket diuretic assay. This is the first instance of a 4-aminopyroglutamate analog of a peptide with a preference for a type VI turn that demonstrates significant bioactivity. The results provide further confirmatory evidence for the active conformation of the insect kinins, and a new scaffold with which to design biostable, peptidomimetic analogs capable of disrupting critical insect kinin-regulated processes in insects. |
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Keywords: | 4‐aminopyroglutamic acid cis‐peptide bond β‐turn mimetic constrained insect kinin analog |
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