TY - JOUR T1 - International Union of Basic and Clinical Pharmacology. XC. Multisite Pharmacology: Recommendations for the Nomenclature of Receptor Allosterism and Allosteric Ligands JF - Pharmacological Reviews JO - Pharmacol Rev SP - 918 LP - 947 DO - 10.1124/pr.114.008862 VL - 66 IS - 4 AU - Arthur Christopoulos AU - Jean-Pierre Changeux AU - William A. Catterall AU - Doriano Fabbro AU - Thomas P. Burris AU - John A. Cidlowski AU - Richard W. Olsen AU - John A. Peters AU - Richard R. Neubig AU - Jean-Philippe Pin AU - Patrick M. Sexton AU - Terry P. Kenakin AU - Frederick J. Ehlert AU - Michael Spedding AU - Christopher J. Langmead A2 - Ohlstein, Eliot H. Y1 - 2014/10/01 UR - http://pharmrev.aspetjournals.org/content/66/4/918.abstract N2 - 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. ER -