Universal Properties and Specificities of the β₂-Adrenergic Receptor-G_s Protein Complex Activation Mechanism Revealed by All-Atom Molecular Dynamics Simulations.

ABSTRACT: G protein-coupled receptors (GPCRs) are transmembrane proteins of high pharmacological relevance. It has been proposed that their activity is linked to structurally distinct, dynamically interconverting functional states and the process of activation relies on an interconnecting network of conformational switches in the transmembrane domain. However, it is yet to be uncovered how ligands with different extents of functional effect exert their actions. According to our recent hypothesis, based on indirect observations and the literature data, the transmission of the external stimulus to the intracellular surface is accompanied by the shift of macroscopic polarization in the transmembrane domain, furnished by concerted movements of highly conserved polar motifs and the rearrangement of polar

SUBMITTER: Mitra A 

PROVIDER: S-EPMC8508748 | biostudies-literature | 2021 Sep

REPOSITORIES: biostudies-literature