Langmead Christopher J
Heptares Therapeutics Ltd, Welwyn Garden City, UK.
Methods Mol Biol. 2011;746:195-209. doi: 10.1007/978-1-61779-126-0_10.
The drive to produce safer and more receptor subtype selective drugs has sparked a renewed interest in allosteric modulators of G protein-coupled receptors. The increasing use of functional assays has shown that allosteric ligands are capable of modulating both orthosteric agonist affinity and efficacy, as well as mediating receptor activation in their own right. Such a complex range of behaviours can be difficult to discern from single datasets; this chapter seeks to explain how to use radioligand binding and functional assay datasets in concert to elucidate allosteric modulator mechanism of action.
生产更安全、更具受体亚型选择性药物的需求引发了对G蛋白偶联受体变构调节剂的新兴趣。功能测定法的日益广泛应用表明，变构配体能够调节正构激动剂的亲和力和效力，并且自身也能介导受体激活。如此复杂的一系列行为可能难以从单一数据集中辨别出来；本章旨在解释如何协同使用放射性配体结合和功能测定数据集来阐明变构调节剂的作用机制。
