The third intracellular loop (ICL3) of the G protein-coupled receptor (GPCR) fold is important
for the signal transduction process downstream of receptor activation,–. Despite this, the lack …

Intrinsically disordered proteins and regions (IDPs and IDRs) and their importance in biology
are becoming increasingly recognized in biology, biochemistry, molecular biology and …

The> 800 human G protein–coupled receptors (GPCRs) are responsible for transducing
diverse chemical stimuli to alter cell state-and are the largest class of drug targets. Their …

Lipids are becoming known as essential allosteric modulators of G protein-coupled receptor
(GPCRs). However, how they exert their effects on GPCR conformation at the atomic level is …

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 …

In recent years, our understanding of function of G protein-coupled receptors (GPCRs) has
changed from a picture of simple signal relays, transmitting only a particular signal to a …

Cannabinoid receptor 1 (CB1) mediates the functional responses of Δ9-
tetrahydrocannabinol. Although progress has been made in understanding cannabinoid …

Biased ligands selectively activating specific downstream signaling pathways (termed as
biased activation) exhibit significant therapeutic potential. However, the conformational …

As class C GPCRs and regulators of synaptic activity, human metabotropic glutamate
receptors (mGluRs) 4 and 5 are prime targets for allosteric modulation, with mGlu5 inhibition …

This study investigates the structural distinctiveness of orthosteric ligand‐binding sites of
several human β2 adrenergic receptor (β2‐AR) conformations that have been obtained from …