Goldsworthy Graham J, Chung J Sook, Simmonds Monique S J, Tatari Maria, Varouni Sophia, Poulos Constantine P
Department of Biology, Birkbeck College, University of London, Malet Street, WC1E 7HX, London, UK.
Peptides. 2003 Oct;24(10):1607-13. doi: 10.1016/j.peptides.2003.09.010.
The synthesis is described of an analogue of the locust CRF-like diuretic peptide in which methionine in positions 1,3, and 13 is replaced by isosteric methyl-homoserine residues. This analogue has been tested for biological activity on Malpighian tubules in vitro, and feeding behavior in vivo. It is highly active in stimulating fluid secretion and accumulation of cAMP in tubules, and on increasing the latency to feed and reducing meal duration. A 15 residue fragment from the C-terminus of the CRF-like peptide, Locmi-DP(32-46), is fully active in the feeding assay, but has only weak ability to stimulate the accumulation of cAMP in tubules. Two smaller fragments, Locmi-DP(32-37) and Locmi-DP(41-46), were tested but neither had consistent biological activity in any of the assays used here. None of the peptides tested have any substantive activity in increasing cGMP in tubules.
描述了一种蝗虫促肾上腺皮质激素释放因子(CRF)样利尿肽类似物的合成,其中第1、3和13位的甲硫氨酸被等排甲基高丝氨酸残基取代。已对该类似物进行体外马氏管生物活性以及体内摄食行为测试。它在刺激小管中液体分泌和环磷酸腺苷(cAMP)积累方面具有高活性,并且在增加摄食潜伏期和缩短进食持续时间方面也有活性。来自CRF样肽C端的一个15个残基的片段Locmi-DP(32 - 46)在摄食试验中具有完全活性,但刺激小管中cAMP积累的能力较弱。测试了两个较小的片段Locmi-DP(32 - 37)和Locmi-DP(41 - 46),但在此处使用的任何试验中它们都没有一致的生物活性。所测试的肽均未在增加小管中环鸟苷酸(cGMP)方面具有任何实质性活性。