Biochemical Pharmacology volume 81, issue 6, P691-702 2011 DOI: 10.1016/j.bcp.2010.12.012 View full text
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Neil T. Burford, John Watson, Robert Bertekap, Andrew Alt

Abstract: Once considered a pharmacological curiosity, allosteric modulation of seven transmembrane domain G-protein-coupled receptors (GPCRs) has emerged as a potentially powerful means to affect receptor function for therapeutic purposes. Allosteric modulators, which interact with binding sites topologically distinct from the orthosteric ligand binding sites, can potentially provide improved selectivity and safety, along with maintenance of spatial and temporal aspects of GPCR signaling. Accordingly, drug discovery ef…

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