RT Journal Article SR Electronic 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 FD American Society for Pharmacology and Experimental Therapeutics SP 918 OP 947 DO 10.1124/pr.114.008862 VO 66 IS 4 A1 Arthur Christopoulos A1 Jean-Pierre Changeux A1 William A. Catterall A1 Doriano Fabbro A1 Thomas P. Burris A1 John A. Cidlowski A1 Richard W. Olsen A1 John A. Peters A1 Richard R. Neubig A1 Jean-Philippe Pin A1 Patrick M. Sexton A1 Terry P. Kenakin A1 Frederick J. Ehlert A1 Michael Spedding A1 Christopher J. Langmead A2 Eliot H. Ohlstein YR 2014 UL http://pharmrev.aspetjournals.org/content/66/4/918.abstract AB 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.