title: Structure-activity relationships for inhibitory insect myosuppressins: contrast with the stimulatory sulfakinins.
abstract: Unusual among insect neuropeptides, the decapeptide myosuppressins are capable of inhibiting contractions of visceral muscle, including the isolated cockroach hindgut. The C-terminal pentapeptide Val-Phe-Leu-Arg-Phe-NH2 has been identified as the myosuppressin active core, the minimum number of residues required to elicit hindgut myoinhibitory activity. Activity of the same magnitude as the parent neuropeptide requires the C-terminal heptapeptide fragment Asp-His-Val-Phe-Leu-Arg-Phe-NH2. Evaluation of a series of substitution analogs delineates structural features critical for myoinhibitory activity within this important fragment. The branched, hydrophobic residues in myosuppressin position 6 (Val) and particularly position 8 (Leu), their absence in the myostimulatory sulfakinins, and the different roles played by the shared Asp residue (myosuppressin position 4; leucosulfakinin position 5) in peptide-receptor interaction, account in large degree for the contrasting biological activities elicited by these otherwise structurally similar peptide families. The results may have broad significance for other invertebrate myotropic systems, such as the locust heart and the pharyngeal retractor muscle of the mollusc Helix aspersa.
authors.affiliation: U.S. Department of Agriculture, Agricultural Research Service, Food Animal Protection Research Laboratory, College Station, TX 77845.
authors.forename: R J
authors.initials: RJ
authors.lastname: Nachman
authors.forename: G M
authors.initials: GM
authors.lastname: Holman
authors.forename: T K
authors.initials: TK
authors.lastname: Hayes
authors.forename: R C
authors.initials: RC
authors.lastname: Beier
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D003058:Cockroaches / Q000378:metabolism*; D007301:Insect Hormones / Q000378:metabolism*; D007413:Intestinal Mucosa / Q000378:metabolism; D008969:Molecular Sequence Data; D009479:Neuropeptides / Q000378:metabolism*; D018013:Receptors, Neuropeptide / Q000378:metabolism*; D017386:Sequence Homology, Amino Acid; D013329:Structure-Activity Relationship
chemical_list: D007301:Insect Hormones; D009479:Neuropeptides; D018013:Receptors, Neuropeptide; C083927:leucomyosuppressin receptor; C058650:leucomyosuppressin