Article
Generation of an agonistic binding site for blockers of the M(3) muscarinic acetylcholine receptor.
The Biochemical journal - 15 May 2008
Thor Doreen, Schulz Angela, Hermsdorf Thomas, Schöneberg Torsten
Abstract excerpt
GPCRs (G-protein-coupled receptors) exist in a spontaneous equilibrium between active and inactive conformations that are stabilized by agonists and inverse agonists respectively. Because ligand binding of agonists and inverse agonists often occurs in a competitive manner, one can assume an overlap between both binding sites. Only a few studies report mutations in GPCRs that convert receptor blockers into...
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