Mechanisms of signalling and biased agonism in G protein-coupled receptors
D Wootten, A Christopoulos, M Marti-Solano… - … reviews Molecular cell …, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest group of cell surface receptors in
humans that signal in response to diverse inputs and regulate a plethora of cellular …
humans that signal in response to diverse inputs and regulate a plethora of cellular …
Structure and dynamics of GPCR signaling complexes
G-protein-coupled receptors (GPCRs) relay numerous extracellular signals by triggering
intracellular signaling through coupling with G proteins and arrestins. Recent breakthroughs …
intracellular signaling through coupling with G proteins and arrestins. Recent breakthroughs …
[HTML][HTML] Structure of a hallucinogen-activated Gq-coupled 5-HT2A serotonin receptor
Hallucinogens like lysergic acid diethylamide (LSD), psilocybin, and substituted N-benzyl
phenylalkylamines are widely used recreationally with psilocybin being considered as a …
phenylalkylamines are widely used recreationally with psilocybin being considered as a …
Signaling snapshots of a serotonin receptor activated by the prototypical psychedelic LSD
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 …
targets for lysergic acid diethylamide (LSD) and all other psychedelic drugs. Although the …
Structures of the entire human opioid receptor family
Opioids are effective analgesics, but their use is beset by serious side effects, including
addiction and respiratory depression, which contribute to the ongoing opioid crisis. The …
addiction and respiratory depression, which contribute to the ongoing opioid crisis. 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 …
Activation pathway of a G protein-coupled receptor uncovers conformational intermediates as targets for allosteric drug design
S Lu, X He, Z Yang, Z Chai, S Zhou, J Wang… - Nature …, 2021 - nature.com
G protein-coupled receptors (GPCRs) are the most common proteins targeted by approved
drugs. A complete mechanistic elucidation of large-scale conformational transitions …
drugs. A complete mechanistic elucidation of large-scale conformational transitions …
ProLIF: a library to encode molecular interactions as fingerprints
C Bouysset, S Fiorucci - Journal of cheminformatics, 2021 - Springer
Interaction fingerprints are vector representations that summarize the three-dimensional
nature of interactions in molecular complexes, typically formed between a protein and a …
nature of interactions in molecular complexes, typically formed between a protein and a …
Structural basis of tethered agonism of the adhesion GPCRs ADGRD1 and ADGRF1
X Qu, N Qiu, M Wang, B Zhang, J Du, Z Zhong, W Xu… - Nature, 2022 - nature.com
Adhesion G protein-coupled receptors (aGPCRs) are essential for a variety of physiological
processes such as immune responses, organ development, cellular communication …
processes such as immune responses, organ development, cellular communication …
Impact of GPCR structures on drug discovery
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 …