Article
Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs.
Nature - 14 Nov 2013
Dror Ron O, Green Hillary F, Valant Celine, Borhani David W, Valcourt James R, Pan Albert C, Arlow Daniel H, Canals Meritxell, Lane J Robert, Rahmani Raphaël, Baell Jonathan B, Sexton Patrick M, Christopoulos Arthur, Shaw David E
Abstract excerpt
The design of G-protein-coupled receptor (GPCR) allosteric modulators, an active area of modern pharmaceutical research, has proved challenging because neither the binding modes nor the molecular mechanisms of such drugs are known. Here we determine binding sites, bound conformations and specific drug-receptor interactions for several allosteric modulators of the M2 muscarinic acetylcholine receptor (M2...
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