Allosteric interactions play vital roles in metabolic processes and signal transduction and, more recently, have become the focus of numerous pharmacological studies because of the potential for discovering more target-selective chemical probes and therapeutic agents. In addition to classic early studies on enzymes, there are now examples of small molecule allosteric modulators for all superfamilies of receptors encoded by the genome, including ligand- and voltage-gated ion channels, G protein-coupled receptors, nuclear hormone receptors, and receptor tyrosine kinases. As a consequence, a vast array of pharmacologic behaviors has been ascribed to allosteric ligands that can vary in a target-, ligand-, and cell-/tissue-dependent manner. The current article presents an overview of allostery as applied to receptor families and approaches for detecting and validating allosteric interactions and gives recommendations for the nomenclature of allosteric ligands and their properties.

中文翻译：

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国际基础与临床药理学联盟。 XC。多位点药理学：受体变构和变构配体命名的建议。


变构相互作用在代谢过程和信号转导中发挥着至关重要的作用，最近，由于有可能发现更多的靶点选择性化学探针和治疗剂，变构相互作用已成为众多药理学研究的焦点。除了关于酶的经典早期研究之外，现在还有针对基因组编码的所有受体超家族的小分子变构调节剂的例子，包括配体门控和电压门控离子通道、G 蛋白偶联受体、核激素受体和受体酪氨酸激酶。因此，大量的药理行为被归因于变构配体，这些配体可以以靶标、配体和细胞/组织依赖性方式变化。本文概述了应用于受体家族的变构以及检测和验证变构相互作用的方法，并为变构配体的命名法及其特性提供了建议。