Weaver C David
Vanderbilt University School of Medicine, Nashville, Tennessee.
Curr Protoc Chem Biol. 2011 Sep 1;3(3):119-40. doi: 10.1002/9780470559277.ch110060.
The detection and characterization of seven-transmembrane-receptor modulators (orthosteric binding site agonists, antagonists, and more recently allosteric modulators) is an area of intense interest for both drug discovery and basic research. Traditionally, assays used to detect and characterize these different modes of modulation have been executed as separate, discrete protocols focused on a particular mode of action (e.g., agonism). In recent years, investigators have begun to combine aspects of these separate protocols to produce methods that detect multiple modes of modulation simultaneously. The power of such approaches is revealed not only in conservation of time and resources, but more importantly in a superior ability to discover and characterize novel modulators of the targets of interest. The protocols in this article describe a general procedure for developing, validating, and utilizing triple-addition assays to enable the simultaneous detection and characterization of multiple modes of seven-transmembrane-receptor modulation. Curr. Protoc. Chem. Biol. 3:119-140 © 2011 by John Wiley & Sons, Inc.
七跨膜受体调节剂（正构结合位点激动剂、拮抗剂以及最近的变构调节剂）的检测与特性分析，是药物研发和基础研究都极为关注的领域。传统上，用于检测和表征这些不同调节模式的测定法，都是作为专注于特定作用模式（如激动作用）的独立、离散方案来执行的。近年来，研究人员已开始将这些独立方案的各个方面结合起来，以产生能同时检测多种调节模式的方法。此类方法的优势不仅体现在节省时间和资源上，更重要的是，在发现和表征目标靶点新型调节剂方面具有更强的能力。本文中的方案描述了开发、验证和利用三重添加测定法的一般程序，以实现对七跨膜受体多种调节模式的同时检测和表征。《化学与生物学实验指南》第3卷：119 - 140页 2011年 约翰威立国际出版公司版权所有
