G protein-coupled receptors (GPCRs) are the most intensively studied drug targets, mostly
due to their substantial involvement in human pathophysiology and their pharmacological …

The 826 G protein-coupled receptors (GPCRs) in the human proteome regulate key
physiological processes and thus have long been attractive drug targets. With the crystal …

In classical G-protein-coupled receptor (GPCR) activation, GPCRs couple to a variety of
heterotrimeric G proteins on the membrane and then activate downstream signaling …

Immune-mediated inflammatory diseases (IMIDs) encompass a wide range of seemingly
unrelated conditions, such as multiple sclerosis, rheumatoid arthritis, psoriasis, inflammatory …

Highlights•GPCRs are key players in cell-cell communication and pass the signal via
coordinated action of switches.•There are two types of switches: toggle switches and …

G protein-coupled receptor (GPCR)-biased agonism, selective activation of certain signaling
pathways relative to others, is thought to be directed by differential GPCR phosphorylation" …

G protein-coupled receptors (GPCRs) are the largest class of membrane receptors, playing
a key role in the regulation of processes as varied as neurotransmission and immune …

Highlights•μ-OR biased agonists represent promising analgesics with improved therapeutic
profiles.•Protein-ligand interactions might account for biased ligands functional …

Orexin-producing neurons in the lateral hypothalamus are a critical regulator of sleep/wake
states, and their loss is associated with narcolepsy type 1 (NT1). Orexin peptides act on two …

α1‐Adrenoceptors are seven transmembrane domain GPCRs involved in numerous
physiological functions controlled by the endogenous catecholamines, noradrenaline and …