G protein-coupled receptors: structure-and function-based drug discovery

D Yang, Q Zhou, V Labroska, S Qin… - Signal transduction and …, 2021 - nature.com
As one of the most successful therapeutic target families, G protein-coupled receptors
(GPCRs) have experienced a transformation from random ligand screening to knowledge …

Serial femtosecond crystallography

TRM Barends, B Stauch, V Cherezov… - Nature Reviews …, 2022 - nature.com
With the advent of X-ray free-electron lasers (XFELs), new, high-throughput serial
crystallography techniques for macromolecular structure determination have emerged …

GPCR activation and GRK2 assembly by a biased intracellular agonist

J Duan, H Liu, F Zhao, Q Yuan, Y Ji, X Cai, X He, X Li… - Nature, 2023 - nature.com
Phosphorylation of G-protein-coupled receptors (GPCRs) by GPCR kinases (GRKs)
desensitizes G-protein signalling and promotes arrestin signalling, which is also modulated …

Common activation mechanism of class A GPCRs

Q Zhou, D Yang, M Wu, Y Guo, W Guo, L Zhong, X Cai… - Elife, 2019 - elifesciences.org
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …

[HTML][HTML] Signaling snapshots of a serotonin receptor activated by the prototypical psychedelic LSD

C Cao, X Barros-Álvarez, S Zhang, K Kim, MA Dämgen… - Neuron, 2022 - cell.com
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 …

GPCR signaling regulation: the role of GRKs and arrestins

VV Gurevich, EV Gurevich - Frontiers in pharmacology, 2019 - frontiersin.org
Every animal species expresses hundreds of different G protein-coupled receptors (GPCRs)
that respond to a wide variety of external stimuli. GPCRs-driven signaling pathways are …

Structure and dynamics of GPCR signaling complexes

D Hilger, M Masureel, BK Kobilka - Nature structural & molecular …, 2018 - nature.com
G-protein-coupled receptors (GPCRs) relay numerous extracellular signals by triggering
intracellular signaling through coupling with G proteins and arrestins. Recent breakthroughs …

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 …

G protein-coupled receptors: a century of research and discovery

S Liu, PJ Anderson, S Rajagopal, RJ Lefkowitz… - Circulation …, 2024 - ahajournals.org
GPCRs (G protein-coupled receptors), also known as 7 transmembrane domain receptors,
are the largest receptor family in the human genome, with≈ 800 members. GPCRs regulate …

Biased signalling: from simple switches to allosteric microprocessors

JS Smith, RJ Lefkowitz, S Rajagopal - Nature reviews Drug discovery, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest class of receptors in the human
genome and some of the most common drug targets. It is now well established that GPCRs …