Ligand Pharmaceuticals, 3000 Eastpark Blvd., Cranbury, NJ 08512, USA.
Curr Pharm Biotechnol. 2010 Nov;11(7):757-63. doi: 10.2174/138920110792927775.
G protein-coupled receptors represent one of the largest families of drug targets. Time and cost may be saved if GPCR modulators are assessed in terms of signaling pathway selectivity, species selectivity, and selectivity against closely-related family members early in the drug discovery process, perhaps even at the stage of high-throughput screening. Examples are given of how these kinds of selectivity have been addressed during screening.
G 蛋白偶联受体是最大的药物靶点家族之一。如果在药物发现过程的早期，甚至在高通量筛选阶段，就根据信号通路选择性、物种选择性和对密切相关家族成员的选择性来评估 GPCR 调节剂，那么可以节省时间和成本。本文举例说明了在筛选过程中如何解决这些选择性问题。
