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 …
Conformational basis of G protein-coupled receptor signaling versatility
LM Wingler, RJ Lefkowitz - Trends in cell biology, 2020 - cell.com
G protein-coupled receptors (GPCRs) are privileged structural scaffolds in biology that have
the versatility to regulate diverse physiological processes. Interestingly, many GPCR ligands …
the versatility to regulate diverse physiological processes. Interestingly, many GPCR ligands …
Insights into distinct signaling profiles of the µOR activated by diverse agonists
Drugs targeting the μ-opioid receptor (μOR) are the most effective analgesics available but
are also associated with fatal respiratory depression through a pathway that remains …
are also associated with fatal respiratory depression through a pathway that remains …
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 …
Identification of 5-HT2A receptor signaling pathways associated with psychedelic potential
Serotonergic psychedelics possess considerable therapeutic potential. Although 5-HT2A
receptor activation mediates psychedelic effects, prototypical psychedelics activate both 5 …
receptor activation mediates psychedelic effects, prototypical psychedelics activate both 5 …
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 …
Molecular mechanism of biased signaling at the kappa opioid receptor
The κ-opioid receptor (KOR) has emerged as an attractive drug target for pain management
without addiction, and biased signaling through particular pathways of KOR may be key to …
without addiction, and biased signaling through particular pathways of KOR may be key to …
Heterotrimeric Gq proteins act as a switch for GRK5/6 selectivity underlying β-arrestin transducer bias
K Kawakami, M Yanagawa, S Hiratsuka… - Nature …, 2022 - nature.com
Signaling-biased ligands acting on G-protein-coupled receptors (GPCRs) differentially
activate heterotrimeric G proteins and β-arrestins. Although a wealth of structural knowledge …
activate heterotrimeric G proteins and β-arrestins. Although a wealth of structural knowledge …
Ligand and G-protein selectivity in the κ-opioid receptor
The κ-opioid receptor (KOR) represents a highly desirable therapeutic target for treating not
only pain but also addiction and affective disorders. However, the development of KOR …
only pain but also addiction and affective disorders. However, the development of KOR …
Structural basis of sphingosine-1-phosphate receptor 1 activation and biased agonism
Abstract Sphingosine-1-phosphate receptor 1 (S1PR1) is a master regulator of lymphocyte
egress from the lymph node and an established drug target for multiple sclerosis (MS) …
egress from the lymph node and an established drug target for multiple sclerosis (MS) …