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

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

Summary Serotonin (5-hydroxytryptamine [5-HT]) 5-HT2-family receptors represent essential
targets for lysergic acid diethylamide (LSD) and all other psychedelic drugs. Although the …

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

Discovered more than 30 years ago, the angiotensin AT2 receptor (AT2R) has evolved from
a binding site with unknown function to a firmly established major effector within the …

Given the promising clinical value of allosteric modulators of G protein-coupled-receptors
(GPCRs), mechanistic understanding of how these modulators alter GPCR function is of …

Over one-third of current drugs target G-protein-coupled receptors (GPCRs). Leveraging the
phenomenon of biased signaling, where different ligands that bind to the same GPCR …

Signaling-biased ligands acting on G-protein-coupled receptors (GPCRs) differentially
activate heterotrimeric G proteins and β-arrestins. Although a wealth of structural knowledge …

Abstract Sphingosine-1-phosphate receptor 1 (S1PR1) is a master regulator of lymphocyte
egress from the lymph node and an established drug target for multiple sclerosis (MS) …

G protein–coupled receptors engage both G proteins and β-arrestins, and their coupling can
be biased by ligands and mutations. Here, to resolve structural elements and mechanisms …