High-Throughput Interrogation of Ligand Binding Mode Using a Fluorescence-Based Assay

被引：26

作者：

Sledz, Pawel ^{[1
]}

Lang, Steffen ^{[1
]}

Stubbs, Christopher J. ^{[1
]}

Abell, Chris ^{[1
]}

机构：

[1] Univ Cambridge, Univ Chem Lab, Cambridge CB2 1EW, England

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2012年 / 51卷 / 31期

基金：

英国惠康基金;

关键词：

binding mode; drug discovery; ligand design; protein structures; structure-activity relationships; POLO-BOX DOMAIN; TUBERCULOSIS PANTOTHENATE SYNTHETASE; KINASE; FRAGMENT LINKING; DISCOVERY; IDENTIFICATION;

D O I：

10.1002/anie.201202660

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Probing the pocket: A high-throughput fluorescence-based thermal shift (FTS) assay utilized different forms of a protein (in gray) to establish the binding mode of a ligand (see picture). The assay serves in the rapid evaluation of structure-activity binding-mode relationships for a series of ligands of Plk1, an important target of anticancer therapy. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

引用

页码：7680 / 7683

页数：4

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