Receptor assay guided structure-activity studies of helicokinin insect neuropeptides and peptidomimetic analogues

✍ Scribed by Jürgen Scherkenbeck; Horst-Peter Antonicek; Kathrin Vogelsang; Tino Zdobinsky; Karin Brücher; Denise Rehländer; Heru Chen

• Book ID: 105359810
• Publisher: John Wiley and Sons
• Year: 2009
• Tongue: English
• Weight: 140 KB
• Volume: 15
• Category: Article
• ISSN: 1075-2617
• DOI: 10.1002/psc.1176

✦ Synopsis

Abstract

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. Copyright © 2009 European Peptide Society and John Wiley & Sons, Ltd.