Converting Teixobactin into a Cationic Antimicrobial Peptide (AMP)
Converting Teixobactin into a Cationic Antimicrobial Peptide (AMP)
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DOI：
10.1021/acs.jmedchem.7b00834
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发表时间：
2017-09-14
影响因子：
7.3
通讯作者：
de la Torre, Beatriz G.
中科院分区：
文献类型：
--
作者：
Monaim, Shimaa A. H. Abdel;Ramchuran, Estelle J.;de la Torre, Beatriz G.
Teixobactin 是一种头侧链环缩肽，含有两个正电荷。由于存在胍基异常氨基酸 L-同种异体末端，其中一个出现在循环中，而另一个则位于 N 末端。在此，我们介绍 26 种新的 Teixobactin 类似物，其正电荷数量不断增加。为了微调 Teixobactin 的生物活性，我们研究了阳离子性对 SAP 的影响。这些类似物。维持活性的正电荷的最大数量为三到四个。具有五个正电荷的类似物显示出最低的活性。
Teixobactin is a head to side chain cyclo-depsipeptide that contains two positive charges. One is found in the cycle, as a result of the presence of the guanidino-unusual amino acid L-allo-End, while the other is at the N-terminal. Here we introduce 26 new Teixobactin analogues with an increasing number of positive charges. In an attempt to fine-tune the biological activity of Teixobactin, we examined the effect of cationicity on the SAP. of these analogues. The maximum number of positive charges to maintain the activity are three to four. Analogues with five positive charges show the lowest activity.