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Research Highlights

Nature Reviews Drug Discovery 7, 976–977 (1 December 2008) | doi:10.1038/nrd2770

G-protein-coupled receptors: A novel double act

Charlotte Harrison

Many G-protein-coupled receptors (GPCRs) possess two ligand binding sites: an orthosteric site to which endogenous ligands bind, and an allosteric site to which modulators can bind to alter the biological properties of the orthosteric ligand. However, most allosteric modulators lack signalling efficacy in their own right.