title: Inhibition of PK/PBAN-mediated functions in insects: discovery of selective and non-selective inhibitors.
abstract: The antagonistic properties of a few linear and backbone cyclic (BBC) conformationally constraint peptide libraries and their analogs, were tested for the ability to inhibit pyrokinin/pheromone biosynthesis activating neuropeptide (PK/PBAN) mediated functions: sex pheromone biosynthesis in Heliothis peltigera female moths, cuticular melanization in Spodoptera littoralis larvae, pupariation in the fleshfly Neobellieria bullata and hindgut contraction in Leucophaea maderae, elicited by exogenously injected PBAN, pheromonotropin (PT), leucopyrokinin (LPK), myotropin (MT) or by the endogenous peptides. The data revealed differential inhibitory patterns within the same assay with different elicitors (in both the pheromonotropic and melanotropic assays) and among the different functions and disclosed selective antagonists, hinting at the possibility that the receptors that mediate those functions may differ from one another structurally.
authors.affiliation: Department of Entomology, The Volcani Center, Bet Dagan 50250, Israel. vinnie2@agri.gov.il
authors.forename: Miriam
authors.initials: M
authors.lastname: Altstein
authors.forename: Orna
authors.initials: O
authors.lastname: Ben-Aziz
authors.forename: Irina
authors.initials: I
authors.lastname: Zeltser
authors.forename: Kalpana
authors.initials: K
authors.lastname: Bhargava
authors.forename: Michael
authors.initials: M
authors.lastname: Davidovitch
authors.forename: Allison
authors.initials: A
authors.lastname: Strey
authors.forename: Nan
authors.initials: N
authors.lastname: Pryor
authors.forename: Ronald J
authors.initials: RJ
authors.lastname: Nachman
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D005260:Female; D066298:In Vitro Techniques; D007313:Insecta / Q000187:drug effects* / Q000235:genetics / Q000254:growth & development / Q000378:metabolism*; D008297:Male; D008543:Melanins / Q000096:biosynthesis; D009119:Muscle Contraction / Q000187:drug effects; D009479:Neuropeptides / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D009842:Oligopeptides / Q000235:genetics / Q000494:pharmacology; D019151:Peptide Library; D011679:Pupa / Q000187:drug effects; D012724:Sex Attractants / Q000096:biosynthesis
chemical_list: D008543:Melanins; D009479:Neuropeptides; D009842:Oligopeptides; D019151:Peptide Library; D012724:Sex Attractants; C079709:pheromone biosynthesis activating neuropeptide, Helicoverpa zea; C079229:pyrokinin