Hewage C M, Jiang L, Parkinson J A, Ramage R, Sadler I H
Department of Chemistry, University of Edinburgh, UK.
J Biomol Struct Dyn. 1998 Oct;16(2):425-35. doi: 10.1080/07391102.1998.10508258.
The solution structure of a synthetic ET(B) selective agonist, ET-1[Cys(Acm)(1,15), Ala3, Leu7, dAsp8, Aib11] has been solved by 1H NMR and molecular modelling studies. Such solution structures of linear modified peptides in aqueous methanol are being used in an ongoing program of research designed to assist in an understanding of the basic structural requirements for the biological activity of vasoconstrictors. The resulting structure of this peptide is characterised by an alpha-helical conformation between residues Leu6-His16 and by N- and C-termini which assume no defined conformation. A knowledge of the solution structures of this and related peptides, which are ET(B) selective agonists, are proving to be important in the understanding of how they interact with the ET(B) receptor.
一种合成的ET(B)选择性激动剂ET-1[Cys(Acm)(1,15)，Ala3，Leu7，dAsp8，Aib11]的溶液结构已通过1H NMR和分子模拟研究得到解析。线性修饰肽在甲醇水溶液中的这种溶液结构正用于一个正在进行的研究项目，该项目旨在帮助理解血管收缩剂生物活性的基本结构要求。该肽的最终结构的特征是Leu6-His16残基之间呈α-螺旋构象，且N端和C端没有确定的构象。事实证明，了解这种及相关肽（它们是ET(B)选择性激动剂）的溶液结构对于理解它们如何与ET(B)受体相互作用非常重要。
