International union of basic and clinical pharmacology. XC. multisite pharmacology: Recommendations for the nomenclature of receptor allosterism and allosteric ligands

Arthur Christopoulos (Lead / Corresponding author), Jean-Pierre Changeux, William A. Catterall, Doriano Fabbro, Thomas P. Burris, John A. Cidlowski, Richard W. Olsen, John A. Peters, Richard R. Neubig, Jean-Philippe Pin, Patrick M. Sexton, Terry P. Kenakin, Frederick J. Ehlert, Michael Spedding, Christopher J. Langmead

    Research output: Contribution to journalArticle

    120 Citations (Scopus)

    Abstract

    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.
    Original languageEnglish
    Pages (from-to)918-947
    Number of pages30
    JournalPharmacological Reviews
    Volume66
    Issue number4
    DOIs
    Publication statusPublished - Oct 2014

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  • Cite this

    Christopoulos, A., Changeux, J-P., Catterall, W. A., Fabbro, D., Burris, T. P., Cidlowski, J. A., Olsen, R. W., Peters, J. A., Neubig, R. R., Pin, J-P., Sexton, P. M., Kenakin, T. P., Ehlert, F. J., Spedding, M., & Langmead, C. J. (2014). International union of basic and clinical pharmacology. XC. multisite pharmacology: Recommendations for the nomenclature of receptor allosterism and allosteric ligands. Pharmacological Reviews, 66(4), 918-947. https://doi.org/10.1124/pr.114.008862