Abstract
G-protein-coupled receptors (GPCRs) are responsible for transducing signals across lipid membranes in cells and are the largest family of targets (∼40%) for currently approved drugs. They exist as dynamic conformational ensembles with multiple inactive and active conformational substates described by an energy landscape model. We investigated ways in which the receptor hydration level and lipid bilayer composition influence the activation of the archetypical GPCR rhodopsin by quantifying the shift in the metarhodopsin equilibrium in native and POPC recombinant membranes by different polyethylene glycol osmolyte solutions.
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