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基于全固相肽合成的方法合成明胶酶生物合成激活肽(GBAP)类似物文库:研究粪肠球菌群体感应信号的构效关系。

An Entirely Solid Phase Peptide Synthesis-Based Strategy for Synthesis of Gelatinase Biosynthesis-Activating Pheromone (GBAP) Analogue Libraries: Investigating the Structure-Activity Relationships of the Enterococcus faecalis Quorum Sensing Signal.

机构信息

Department of Chemistry, University of Nevada, Reno , 1664 North Virginia Street, Reno, Nevada 89557, United States.

出版信息

Org Lett. 2017 Jun 16;19(12):3295-3298. doi: 10.1021/acs.orglett.7b01444. Epub 2017 Jun 7.

Abstract

The development of an entirely solid-phase peptide synthesis (SPPS)-based synthesis of the quorum sensing signal gelatinase biosynthesis-activating pheromone (GBAP) from Enterococcus faecalis is reported. The method was used to prepare three libraries of analogues to investigate the structure-activity relationships (SARs) of the GBAP signal. The SAR studies revealed new characteristics of the GBAP signal and uncovered the most potent quorum sensing activator in E. faecalis known to date.

摘要

本文报道了一种基于全固相肽合成(SPPS)的粪肠球菌群体感应信号明胶酶生物合成激活肽(GBAP)合成方法。该方法用于制备三种类似物文库,以研究 GBAP 信号的结构-活性关系(SAR)。SAR 研究揭示了 GBAP 信号的新特征,并发现了迄今为止在粪肠球菌中已知的最有效的群体感应激活剂。

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