Article
Evolutionary action and structural basis of the allosteric switch controlling β2AR functional selectivity.
Nature communications - 18 Dec 2017
Schönegge Anne-Marie, Gallion Jonathan, Picard Louis-Philippe, Wilkins Angela D, Le Gouill Christian, Audet Martin, Stallaert Wayne, Lohse Martin J, Kimmel Marek, Lichtarge Olivier, Bouvier Michel
Abstract excerpt
Functional selectivity of G-protein-coupled receptors is believed to originate from ligand-specific conformations that activate only subsets of signaling effectors. In this study, to identify molecular motifs playing important roles in transducing ligand binding into distinct signaling responses, we combined in silico evolutionary lineage analysis and structure-guided site-directed mutagenesis with large-scale...
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