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High-Throughput Synthesis and Screening of Cyclic Peptide Antibiotics

Year: 2007
Type: article
Abstract: 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.
DOI: 10.1021/jm070282e
Authors: Qing Xiao, Dehua Pei
Language: English
Open Access status: green
OpenAlex ID: W2051655495
FWCI: 1.439
Cites: 27
Cited by: 58
Related to: 10