Scherkenbeck Jürgen, Antonicek Horst-Peter, Vogelsang Kathrin, Zdobinsky Tino, Brücher Karin, Rehländer Denise, Chen Heru
Fachgruppe Chemie, Bergische Universität Wuppertal, Gaussstrasse 20, D-42119 Wuppertal, Germany.
J Pept Sci. 2009 Nov;15(11):783-9. doi: 10.1002/psc.1176.
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.
神经肽控制昆虫体内众多的生理过程。水分平衡的调节是陆生昆虫体内稳态的一个关键方面，并且已表明其受内分泌控制，主要是由促肾上腺皮质激素释放因子（CRF）相关肽和激肽所调控。对于来自具有经济重要性的害虫烟芽夜蛾的利尿神经肽Helicokinin I，基于截短结构、多样的氨基酸扫描以及拟肽类似物，已经建立了详细的构效关系。将所选化合物在功能性表达的Helicokinin受体上的活性与马氏管测定结果进行比较。还提供了对进一步拟肽变体的启示。
