As one of the most successful therapeutic target families, G protein-coupled receptors
(GPCRs) have experienced a transformation from random ligand screening to knowledge …

Adrenergic receptors are G protein-coupled receptors for epinephrine and norepinephrine.
They are targets of many drugs for various conditions, including treatment of hypertension …

Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …

G protein-coupled receptors (GPCRs) are the most common proteins targeted by approved
drugs. A complete mechanistic elucidation of large-scale conformational transitions …

Allostery is a universal, biological phenomenon in which orthosteric sites are fine‐tuned by
topologically distal allosteric sites triggered by perturbations, such as ligand binding, residue …

G protein-coupled receptors (GPCRs), the largest family of human membrane proteins and
an important class of drug targets, play a role in maintaining numerous physiological …

Increasing data in allostery are requiring analysis of coupling relationships among different
allosteric sites on a single protein. Here, based on our previous efforts on reversed allosteric …

Highlights•Allosteric GPCR drug discovery is gaining increasing attention.•Lipid bilayer
plays a unique role in the allosteric sites of GPCRs.•The role of lipid bilayer in allosteric sites …

G protein-coupled receptors (GPCRs) are versatile and vital proteins involved in a wide
array of physiological processes and responses, such as sensory perception (eg, vision …

Diabetes, a metabolic disease caused by abnormally high levels of blood glucose, has a
high prevalence rate worldwide and causes a series of complications, including coronary …