期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 50, 期 13, 页码 3132-3137出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm070282e
关键词
-
资金
- NIGMS NIH HHS [R01 GM062820-04, GM062820, R01 GM062820, R01 GM062820-05A1] Funding Source: Medline
Cyclic peptides are a rich source of biologically active compounds and are produced in nature by plants, bacteria, fungi, and lower sea animals. A high-throughput methodology has been developed for the combinatorial synthesis, screening, and identification of cyclic peptide natural product analogues with improved biological activities or useful new activities. The methodology was applied to generate a library of 1716 tyrocidine A analogues, which were screened for antibacterial activity in 96-well plates. The identity of the active peptides was determined by partial Edman degradation/mass spectrometry. This has resulted in the discovery of a series of tyrocidine analogues that have significantly improved therapeutic indices compared to the natural product. The availability of tyrocidine analogues with varying antibacterial activities has provided important insights into the structure-function relationship of tyrocidine A, which should help reveal its mechanism of action.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据