A C-terminal aldehyde insect kinin analog enhances inhibition of weight gain and induces significant mortality in Helicoverpa zea larvae

The first reported examples of C-terminal aldehyde analogs of an insect neuropeptide are described. They are hexapeptide insect kinin analogs Boc-VFFPWG-H and Fmoc-RFFPWG-H. Activity observed for these modified analogs in an in vitro insect diuretic assay confirms that the C-terminal aldehyde group...

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Veröffentlicht in:Peptides (New York, N.Y. : 1980) N.Y. : 1980), 2003-10, Vol.24 (10), p.1615-1621
Hauptverfasser: Nachman, Ronald J., Coast, Geoffrey M., Douat, Céline, Fehrentz, Jean-Alain, Kaczmarek, Krzyztoff, Zabrocki, Janusz, Pryor, Nan W., Martinez, Jean
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Sprache:eng
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Zusammenfassung:The first reported examples of C-terminal aldehyde analogs of an insect neuropeptide are described. They are hexapeptide insect kinin analogs Boc-VFFPWG-H and Fmoc-RFFPWG-H. Activity observed for these modified analogs in an in vitro insect diuretic assay confirms that the C-terminal aldehyde group is tolerated by an insect kinin receptor. The two analogs demonstrate greatly enhanced activity over standard C-terminal amide insect kinins in a larval weight gain inhibition assay in the corn earworm Helicoverpa zea. Treatment with Boc-VFFPWG-H led to significant increases in larval mortality at doses of 500 pm (45%) and 5 nm (67%). Boc-VFFPWG-H represents a lead analog in the development of novel, environmentally friendly pest insect management agents based on the insect kinin class of neuropeptides.
ISSN:0196-9781
1873-5169
DOI:10.1016/j.peptides.2003.06.008