Catalysis and Peptide Research Unit, School of Health Sciences, University of KwaZulu-Natal, Durban 4001, South Africa.
Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
Molecules. 2017 Sep 28;22(10):1632. doi: 10.3390/molecules22101632.
Teixobactin is a recently described antimicrobial peptide that shows high activity against gram-positive bacteria as well as . Due to both its structure as a head-to-side chain cyclodepsipeptide and its activity, it has attracted the attention of several research groups. In this regard, a large number of analogs with substitutions in both the cycle and the tail has been described. Here, we report the contribution of the -terminus residue, -Me-d-Phe, to the activity of Arg-teixobactin. On the basis of our findings, we conclude that the -terminus accepts minimum changes but not the presence of long alkyl chains. The presence of a positive charge is a requirement for the activity of the peptide. Furthermore, acylation of the -terminus leads to total loss of activity.
Teixobactin 是一种最近被描述的抗菌肽，对革兰氏阳性菌具有很高的活性。由于其结构为头到侧链环二肽以及其活性，它引起了几个研究小组的关注。在这方面，已经描述了在环和尾部都有取代的大量类似物。在这里，我们报告了 -末端残基 -Me-d-Phe 对 Arg-teixobactin 活性的贡献。根据我们的发现，我们得出结论，-末端接受最小的变化，但不接受长烷基链的存在。正电荷的存在是该肽活性的要求。此外，-末端的酰化会导致完全丧失活性。
