… GPCRs regulate all aspects of human physiology, and … of GPCR conformational regulation
by different ligands. Yet there is no experimental evidence for how sidechain dynamics control …

… GPCRs regulate all aspects of human physiology, and … of GPCR conformational regulation
by different ligands. Yet there is no experimental evidence for how sidechain dynamics control …

… activity when tested with the wild type ligand (first cycle, … , including biased agonists and
allosteric modulators, might … different ligands differently modulate the fast side chain dynamics (ps…

… about GPCR dynamics that is relevant for receptor activation, signalling bias and allosteric
modulation. … ligands, allosteric modulators for GPCRs present a paramount research focus. …

… to wild type … ligand influencing both the initial interaction with an IBP (propensity to bind,
and IBP selectivity) as well as the subsequent signalling activity through modulation of the GPCR…

… of ligands, allosteric modulators, and the membrane environment. This ensemble view of
GPCRs … Fluorine labeling is typically achieved through chemical labeling of cysteine sidechains …

… GPCRs conformations at equilibrium, ie inactive, active and intermediate states, whose
probability and lifetime are modulated by the presence of ligands … of the side-chain of isoleucines …

… of these techniques with studies of human GPCRs in intact cells or even tissues … the dynamic
interplay between the interactions of GPCRs with orthosteric ligands, allosteric modulators, …

… effector of A2AR through modulation of its functional states. … of GPCR conformational
regulation by different ligands. Yet … , we generated samples of a wild-type GPCR (A2AR) that are …

… Allosteric ligands modulate the effect of the orthosteric ligand … differences between wild
type and variant GPCRs, providing … by monitoring the dynamics of sidechain rotations and the …