Receptor assay guided structure-activity studies of helicokinin insect neuropeptides and peptidomimetic analogues.
Neuropeptides control numerous physiological processes in insects. The regulation of water balance is a crucial aspect of homeostasis in terrestrial insects and has been shown to be under endocrine control, primarily by corticotrophin releasing factor (CRF)-related peptides and kinins. For helicokinin I, a diuretic neuropeptide from the economically important insect pest Heliothis virescens, detailed structure-activity relationships have been established based on truncated structures, diverse amino acid scans and peptidomimetic analogues. The activities of selected compounds on functional expressed helicokinin receptors are compared with the results of a Malphigian tubule assay. Implications for further peptidomimetic variations are provided.
Scherkenbeck
Jürgen
J
Fachgruppe Chemie, Bergische Universität Wuppertal, Gaussstrasse 20, D-42119 Wuppertal, Germany. scherkenbeck@uni-wuppertal.de
Antonicek
Horst-Peter
HP
Vogelsang
Kathrin
K
Zdobinsky
Tino
T
Brücher
Karin
K
Rehländer
Denise
D
Chen
Heru
H
D000595:Amino Acid Sequence; D000818:Animals; D019476:Insect Proteins / Q000737:chemistry / Q000378:metabolism; D007313:Insecta / Q000378:metabolism*; D009479:Neuropeptides / Q000737:chemistry* / Q000378:metabolism*; D011485:Protein Binding; D018013:Receptors, Neuropeptide / Q000378:metabolism; D013329:Structure-Activity Relationship
D019476:Insect Proteins; D009479:Neuropeptides; D018013:Receptors, Neuropeptide