Structures of 70 unique G protein-coupled receptors (GPCRs) have been determined, with
over 370 structures in total bound to different ligands and the receptors in various …

Safety and efficacy constitute the major criteria governing regulatory approval of any new
drug. The best method to maximize safety and efficacy is to deliver a proven therapeutic …

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

The adenosine A1 receptor (A1R) is a promising therapeutic target for non-opioid analgesic
agents to treat neuropathic pain,. However, development of analgesic orthosteric A1R …

Allosteric regulation plays an important role in many biological processes, such as signal
transduction, transcriptional regulation, and metabolism. Allostery is rooted in the …

Based upon evidence that the therapeutic properties of C annabis preparations are not
solely dependent upon the presence of Δ9‐tetrahydrocannabinol (THC), pharmacological …

The glucagon-like peptide (GLP)-1 receptor (GLP-1R) is a class BG protein–coupled
receptor (GPCR) that mediates the action of GLP-1, a peptide hormone secreted from three …

Most evidence indicates that, as for family CG protein–coupled receptors (GPCRs), family A
GPCRs form homo-and heteromers. Homodimers seem to be a predominant species, with …

The muscarinic acetylcholine receptors are a subfamily of G protein-coupled receptors that
regulate numerous fundamental functions of the central and peripheral nervous system. The …

Agonists of seven-transmembrane receptors, also known as G protein-coupled receptors
(GPCRs), do not uniformly activate all cellular signalling pathways linked to a given seven …