Bacterial transglycosylases: assays for monitoring the activity using Lipid II substrate analogs and methods for discovering new antibiotics
申请人:——
公开号:US20030129683A1
公开(公告)日:2003-07-10
This invention provides a direct method for monitoring bacterial transglycosylase activity using labeled substrates produced by chemo-enzymatic synthesis wherein the labels are selected to permit the detection of both polymeric and non-polymeric products simultaneously, either directly or following the separation of product from starting material. The invention promotes the discovery of new antibiotics with activity against bacterial transglycosylases by a) laying the groundwork for structural analysis of purified, active transglycosylase (which permits structure-based design); and b) providing an assay that can be used to screen for inhibitors.
本发明提供了一种直接监测细菌转糖基化酶活性的方法,该方法使用化学酶法合成产生的标记底物,其中标记的选择允许同时检测聚合和非聚合产物,可以直接检测,也可以在产物与起始材料分离后检测。本发明通过 a) 为纯化的活性转糖苷酶的结构分析奠定基础(允许基于结构的设计);b) 提供可用于筛选抑制剂的检测方法,从而促进发现对细菌转糖苷酶有活性的新抗生素。