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

Arthur Christopoulos, Jean-Pierre Changeux, William A Catterall, Doriano Fabbro, Thomas P Burris, John A Cidlowski, Richard W Olsen, John A Peters, Richard Neubig, Jean Philippe Pin, Patrick Sexton, Terry P Kenakin, Frederick J Ehlert, Michael Spedding, Christopher J Langmead

Research output: Contribution to journalArticleResearchpeer-review

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 - 2014

Cite this

Christopoulos, Arthur ; Changeux, Jean-Pierre ; Catterall, William A ; Fabbro, Doriano ; Burris, Thomas P ; Cidlowski, John A ; Olsen, Richard W ; Peters, John A ; Neubig, Richard ; Pin, Jean Philippe ; Sexton, Patrick ; Kenakin, Terry P ; Ehlert, Frederick J ; Spedding, Michael ; Langmead, Christopher J. / International union of basic and clinical pharmacology. XC. Multisite pharmacology: Recommendations for the nomenclature of receptor allosterism and allosteric ligands. In: Pharmacological Reviews. 2014 ; Vol. 66, No. 4. pp. 918 - 947.
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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.",
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Christopoulos, A, Changeux, J-P, Catterall, WA, Fabbro, D, Burris, TP, Cidlowski, JA, Olsen, RW, Peters, JA, Neubig, R, Pin, JP, Sexton, P, Kenakin, TP, Ehlert, FJ, Spedding, M & Langmead, CJ 2014, 'International union of basic and clinical pharmacology. XC. Multisite pharmacology: Recommendations for the nomenclature of receptor allosterism and allosteric ligands', Pharmacological Reviews, vol. 66, no. 4, pp. 918 - 947. https://doi.org/10.1124/pr.114.008862

International union of basic and clinical pharmacology. XC. Multisite pharmacology: Recommendations for the nomenclature of receptor allosterism and allosteric ligands. / Christopoulos, Arthur; Changeux, Jean-Pierre; Catterall, William A; Fabbro, Doriano; Burris, Thomas P; Cidlowski, John A; Olsen, Richard W; Peters, John A; Neubig, Richard; Pin, Jean Philippe; Sexton, Patrick; Kenakin, Terry P; Ehlert, Frederick J; Spedding, Michael; Langmead, Christopher J.

In: Pharmacological Reviews, Vol. 66, No. 4, 2014, p. 918 - 947.

Research output: Contribution to journalArticleResearchpeer-review

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AU - Christopoulos, Arthur

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AU - Fabbro, Doriano

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AU - Peters, John A

AU - Neubig, Richard

AU - Pin, Jean Philippe

AU - Sexton, Patrick

AU - Kenakin, Terry P

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