Impact of GPCR structures on drug discovery
M Congreve, C de Graaf, NA Swain, CG Tate - Cell, 2020 - cell.com
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 …
over 370 structures in total bound to different ligands and the receptors in various …
The angiotensin AT2 receptor: from a binding site to a novel therapeutic target
UM Steckelings, RE Widdop, ED Sturrock… - Pharmacological …, 2022 - ASPET
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 …
a binding site with unknown function to a firmly established major effector within the …
Common activation mechanism of class A GPCRs
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …
physiology. Understanding receptor activation mechanism is critical for discovering novel …
Structural insights into the lipid and ligand regulation of serotonin receptors
Abstract Serotonin, or 5-hydroxytryptamine (5-HT), is an important neurotransmitter, that
activates the largest subtype family of G-protein-coupled receptors. Drugs that target 5 …
activates the largest subtype family of G-protein-coupled receptors. Drugs that target 5 …
[HTML][HTML] Structural insights into the human D1 and D2 dopamine receptor signaling complexes
Summary The D1-and D2-dopamine receptors (D1R and D2R), which signal through G s
and G i, respectively, represent the principal stimulatory and inhibitory dopamine receptors …
and G i, respectively, represent the principal stimulatory and inhibitory dopamine receptors …
[HTML][HTML] Illuminating G-protein-coupling selectivity of GPCRs
Heterotrimetic G proteins consist of four subfamilies (G s, G i/o, G q/11, and G 12/13) that
mediate signaling via G-protein-coupled receptors (GPCRs), principally by receptors binding …
mediate signaling via G-protein-coupled receptors (GPCRs), principally by receptors binding …
GPCRs steer Gi and Gs selectivity via TM5-TM6 switches as revealed by structures of serotonin receptors
Summary Serotonin (or 5-hydroxytryptamine, 5-HT) is an important neurotransmitter that
activates 12 different G protein-coupled receptors (GPCRs) through selective coupling of G …
activates 12 different G protein-coupled receptors (GPCRs) through selective coupling of G …
Structure of a signaling cannabinoid receptor 1-G protein complex
Cannabis elicits its mood-enhancing and analgesic effects through the cannabinoid receptor
1 (CB1), a G protein-coupled receptor (GPCR) that signals primarily through the adenylyl …
1 (CB1), a G protein-coupled receptor (GPCR) that signals primarily through the adenylyl …
Cryo-EM structure of the human cannabinoid receptor CB2-Gi signaling complex
Drugs selectively targeting CB2 hold promise for treating neurodegenerative disorders,
inflammation, and pain while avoiding psychotropic side effects mediated by CB1. The …
inflammation, and pain while avoiding psychotropic side effects mediated by CB1. The …
Structures of the M1 and M2 muscarinic acetylcholine receptor/G-protein complexes
Muscarinic acetylcholine receptors are G protein–coupled receptors that respond to
acetylcholine and play important signaling roles in the nervous system. There are five …
acetylcholine and play important signaling roles in the nervous system. There are five …