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Structural Mimicry in Class A G Protein-coupled Receptor Rotamer Toggle Switches
Journal of Biological Chemistry
In this study, we tested the hypothesis that a CB 1 TMH3-4-5-6 aromatic microdomain, which includes F3.25 ( 190), F3.36(201), W5.43(280), and W6.48(357), is centrally involved in CB 1 receptor activation, with the F3.36(201)/W6.48(357) interaction key to the maintenance of the CB 1 -inactive state. We have shown previously that when F3.36(201), W5.43(280), and W6.48(357) are individually mutated to alanine, a significant reduction in ligand binding affinity is observed in the presence of WINdoi:10.1074/jbc.m406648200 pmid:15326174 fatcat:3qmt23uzsbglnarqnvgpqopqva