G Protein-Coupled Receptor Allosterism and Complexing

By Arthur Christopoulos, Terry Kenakin. Pharmacological Reviews, 2002

946 citations recorded by the source corpus.

Subfields: Cellular and Molecular Neuroscience, Molecular Biology

View Paper: https://www.semanticscholar.org/paper/22ea05086643e31b17f8952811fc6332ae921451

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In Cellular and Molecular Neuroscience

In Molecular Biology

Citations in the corpus

Inhibition of Hedgehog signaling by direct binding of cyclopamine to Smoothened. (2002, background): “The structurally related GPCR family uses a conformational change to link the binding of extracellular ligands to the recruitment of intracellular components, in this case G proteins (Christopoulos and Kenakin 2002).”
Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders (2009, background): “The diverse effects on receptor behaviour engendered by allosteric ligands can be described by equations based on various ternary complex mass-action model”
Functional Selectivity and Classical Concepts of Quantitative Pharmacology (2007, background): “One direction for reconciling these experimental observations is to build more complex drug-receptor models that not only accommodate our current understanding of protein biophysics but also incorporate multiple receptor states (Christopoulos and Kenakin, 2002).”
Drugs for allosteric sites on receptors. (2014, background): “In addition to PAMs and NAMs, silent allosteric modulators (SAMs; also known as neutral allosteric ligands) bind at allosteric sites and can block the activity of PAMs and NAMs, yet they have no effect on orthosteric ligand responses (1-14).”
International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on Terms and Symbols in Quantitative Pharmacology (2003, background): “Nomenclature concerning the actions of allosteric (allotopic) ligands is presented based on recent literature (Christopoulos and Kenakin, 2002).”
Allosteric binding sites on cell-surface receptors: novel targets for drug discovery (2002, background): “Although more recent receptor models have been developed to more faithfully reflect the full theoretical spectrum of allosteric effect”
Cannabidiol is a negative allosteric modulator of the cannabinoid CB1 receptor (2015, methodology): “4800 British Journal of Pharmacology (2015) 172 4790–4805 Allosteric modulators are probe-dependent; that is, the activity of the allosteric modulator depends on the orthosteric probe being used (Christopoulos and Kenakin, 2002).”