title: A C-terminal aldehyde insect kinin analog enhances inhibition of weight gain and induces significant mortality in Helicoverpa zea larvae.
abstract: 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 500pm (45%) and 5nm (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.
authors.affiliation: Areawide Pest Management Research, Southern Plains Agricultural Research Center, USDA, 2881 F/B Road, College Station, TX 77845, USA. nachman@tamu.edu
authors.forename: Ronald J
authors.initials: RJ
authors.lastname: Nachman
authors.forename: Geoffrey M
authors.initials: GM
authors.lastname: Coast
authors.forename: Céline
authors.initials: C
authors.lastname: Douat
authors.forename: Jean Alain
authors.initials: JA
authors.lastname: Fehrentz
authors.forename: Krzyztoff
authors.initials: K
authors.lastname: Kaczmarek
authors.forename: Janusz
authors.initials: J
authors.lastname: Zabrocki
authors.forename: Nan W
authors.initials: NW
authors.lastname: Pryor
authors.forename: Jean
authors.initials: J
authors.lastname: Martinez
mesh_terms: D000447:Aldehydes / Q000737:chemistry* / Q000494:pharmacology; D000595:Amino Acid Sequence; D000818:Animals; D001681:Biological Assay; D006135:Gryllidae; D007267:Injections; D019476:Insect Proteins / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D007705:Kinins / Q000737:chemistry* / Q000494:pharmacology*; D007814:Larva / Q000187:drug effects* / Q000254:growth & development / Q000502:physiology; D007915:Lepidoptera / Q000187:drug effects* / Q000254:growth & development / Q000502:physiology; D008317:Malpighian Tubules / Q000187:drug effects / Q000378:metabolism; D009479:Neuropeptides / Q000737:chemistry / Q000494:pharmacology; D015996:Survival Rate; D015430:Weight Gain / Q000187:drug effects*
chemical_list: D000447:Aldehydes; D019476:Insect Proteins; D007705:Kinins; D009479:Neuropeptides