G protein-coupled receptors (GPCRs) are privileged structural scaffolds in biology that have
the versatility to regulate diverse physiological processes. Interestingly, many GPCR ligands …

G protein‐coupled receptors (GPCRs) play critical roles in the regulation of human
physiology in response to a wide array of different extracellular stimuli and thus represent …

Crystallography and cryo-electron microscopy have advanced atomic resolution
perspectives of inactive and active states of G protein-coupled receptors (GPCRs), alone …

A long evolution of knowledge of the psychostimulant caffeine led in the 1960s to another
purine natural product, adenosine and its A2A receptor. Adenosine is a short‐lived …

Over the past decade, the vast amount of information generated through structural and
biophysical studies of GPCRs has provided unprecedented mechanistic insight into the …

Understanding the roles of intermediate states in signaling is pivotal to unraveling the
activation processes of G protein-coupled receptors (GPCRs). However, the field is still …

G protein-coupled receptors (GPCRs) are a large family of integral membrane proteins
which conduct a wide range of biological roles and represent significant drug targets. Most …

G protein–coupled receptors (GPCRs) initiate signaling cascades via G-proteins and beta-
arrestins (βarr). βarr-dependent actions begin with recruitment of βarr to the phosphorylated …

Cholesterol as an allosteric modulator of G protein-coupled receptor (GPCR) function is well
documented. This quintessential mammalian lipid facilitates receptor–ligand interactions …

β2AR is an important drug target protein involving many diseases. Biased drugs induce
specific signaling and provide additional clinical utility to optimize β2AR-based therapies …