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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 …
(GPCRs) have experienced a transformation from random ligand screening to knowledge …
Serial femtosecond crystallography
With the advent of X-ray free-electron lasers (XFELs), new, high-throughput serial
crystallography techniques for macromolecular structure determination have emerged …
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 …
desensitizes G-protein signalling and promotes arrestin signalling, which is also modulated …
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 …
[HTML][HTML] 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 …
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 …
that respond to a wide variety of external stimuli. GPCRs-driven signaling pathways are …
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 …
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 …
G protein-coupled receptors: a century of research and discovery
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 …
are the largest receptor family in the human genome, with≈ 800 members. GPCRs regulate …
Biased signalling: from simple switches to allosteric microprocessors
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 …
genome and some of the most common drug targets. It is now well established that GPCRs …