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 …
Improved tools to study astrocytes
Astrocytes are a type of glial cell that tile the CNS. They interact with multiple cell types,
including neurons, glial cells and blood vessels, and are involved or implicated in brain …
including neurons, glial cells and blood vessels, and are involved or implicated in brain …
GPCRdb in 2021: integrating GPCR sequence, structure and function
AJ Kooistra, S Mordalski… - Nucleic Acids …, 2021 - academic.oup.com
G protein-coupled receptors (GPCRs) form both the largest family of membrane proteins and
drug targets, mediating the action of one-third of medicines. The GPCR database, GPCRdb …
drug targets, mediating the action of one-third of medicines. The GPCR database, GPCRdb …
[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 …
Receptor-associated independent cAMP nanodomains mediate spatiotemporal specificity of GPCR signaling
SE Anton, C Kayser, I Maiellaro, K Nemec, J Möller… - Cell, 2022 - cell.com
G protein-coupled receptors (GPCRs) relay extracellular stimuli into specific cellular
functions. Cells express many different GPCRs, but all these GPCRs signal to only a few …
functions. Cells express many different GPCRs, but all these GPCRs signal to only a few …
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 …
TRUPATH, an open-source biosensor platform for interrogating the GPCR transducerome
G-protein-coupled receptors (GPCRs) remain major drug targets, despite our incomplete
understanding of how they signal through 16 non-visual G-protein signal transducers …
understanding of how they signal through 16 non-visual G-protein signal transducers …
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 …
Structure of the neurotensin receptor 1 in complex with β-arrestin 1
Arrestin proteins bind to active, phosphorylated G-protein-coupled receptors (GPCRs),
thereby preventing G-protein coupling, triggering receptor internalization and affecting …
thereby preventing G-protein coupling, triggering receptor internalization and affecting …
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 …