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.
Fachgruppe Chemie, Bergische Universität Wuppertal, Gaussstrasse 20, D-42119 Wuppertal, Germany. scherkenbeck@uni-wuppertal.de
Jürgen
J
Scherkenbeck
Horst-Peter
HP
Antonicek
Kathrin
K
Vogelsang
Tino
T
Zdobinsky
Karin
K
Brücher
Denise
D
Rehländer
Heru
H
Chen
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