Simonsen Shane M, Daly Norelle L, Craik David J
Institute for Molecular Bioscience, University of Queensland, Brisbane, Qld. 4072, Australia.
FEBS Lett. 2004 Nov 19;577(3):399-402. doi: 10.1016/j.febslet.2004.10.034.
The cyclotides are a family of head-to-tail cyclized peptides that display exceptionally high stability and a range of biological activities. Acyclic permutants that contain a break in the circular backbone have been reported to be devoid of the haemolytic activity of the prototypic cyclotide kalata B1, but the potential role of the charges at the introduced termini in this loss of membraneolytic activity has not been fully determined. In this study, acyclic permutants of kalata B1 with capped N- and C-termini were synthesized and found to adopt a native fold. These variants were observed to cause no measurable lysis of erythrocytes, strengthening the connection between backbone cyclization and haemolytic activity.
环肽是一类头对尾环化的肽，具有极高的稳定性和一系列生物活性。据报道，在环状主链上有一处断裂的非环化置换变体不具有原型环肽卡拉塔B1的溶血活性，但引入末端电荷在这种膜溶解活性丧失中的潜在作用尚未完全确定。在本研究中，合成了N端和C端封闭的卡拉塔B1非环化置换变体，发现其具有天然折叠结构。观察到这些变体不会引起可测量的红细胞裂解，这加强了主链环化与溶血活性之间的联系。
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