Inhibition of PK/PBAN-mediated functions in insects: Discovery of selective and non-selective inhibitors

• Published in: Peptides (New York, N.Y. : 1980) Vol. 28; no. 3; pp. 574 - 584
• Main Authors: Altstein, Miriam, Ben-Aziz, Orna, Zeltser, Irina, Bhargava, Kalpana, Davidovitch, Michael, Strey, Allison, Pryor, Nan, Nachman, Ronald J.
• Format: Journal Article
• Language: English
• Published: New York, NY Elsevier Inc 01.03.2007; Elsevier Science
• Subjects: Amino Acid Sequence; Animals; Biological and medical sciences; Cuticular melanization; Female; Fundamental and applied biological sciences. Psychology; Hindgut contraction; In Vitro Techniques; Insect neuropeptide antagonists; Insecta - drug effects; Insecta - genetics; Insecta - growth & development; Insecta - metabolism; Male; Melanins - biosynthesis; Muscle Contraction - drug effects; Neuropeptides - antagonists & inhibitors; Neuropeptides - genetics; Neuropeptides - metabolism; Oligopeptides - genetics; Oligopeptides - pharmacology; PBAN; Peptide Library; Pupa - drug effects; Pupariation; Sex Attractants - biosynthesis; Sex pheromone biosynthesis; Vertebrates: endocrinology; PBAN; Sex pheromone biosynthesis; Pupariation; Insect neuropeptide antagonists; Hindgut contraction; Cuticular melanization; Sex pheromone; Insecta; Biosynthesis; Neuropeptide; Arthropoda; Antagonist; Inhibition; Invertebrata
• ISSN: 0196-9781; 1873-5169
• DOI: 10.1016/j.peptides.2006.11.018

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.