Community guidelines for GPCR ligand bias: IUPHAR review 32
P Kolb, T Kenakin, SPH Alexander… - British journal of …, 2022 - Wiley Online Library
GPCRs modulate a plethora of physiological processes and mediate the effects of one‐third
of FDA‐approved drugs. Depending on which ligand activates a receptor, it can engage …
of FDA‐approved drugs. Depending on which ligand activates a receptor, it can engage …
Neuronal G protein-gated K+ channels
H Luo… - American Journal of …, 2022 - journals.physiology.org
G protein-gated inwardly rectifying K+ (GIRK/Kir3) channels exert a critical inhibitory
influence on neurons. Neuronal GIRK channels mediate the G protein-dependent …
influence on neurons. Neuronal GIRK channels mediate the G protein-dependent …
GLP-1R signaling neighborhoods associate with the susceptibility to adverse drug reactions of incretin mimetics
G protein-coupled receptors are important drug targets that engage and activate signaling
transducers in multiple cellular compartments. Delineating therapeutic signaling from …
transducers in multiple cellular compartments. Delineating therapeutic signaling from …
Subcellular location defines GPCR signal transduction
A Radoux-Mergault, L Oberhauser, S Aureli… - Science …, 2023 - science.org
Intracellular G protein-coupled receptors (GPCRs) can be activated by permeant ligands,
which contributes to agonist selectivity. Opioid receptors (ORs) provide a notable example …
which contributes to agonist selectivity. Opioid receptors (ORs) provide a notable example …
Conformation-and activation-based BRET sensors differentially report on GPCR–G protein coupling
SC Wright, C Avet, SA Gaitonde, I Muneta-Arrate… - Science …, 2024 - science.org
G protein–coupled receptors (GPCRs) regulate cellular signaling processes by coupling to
diverse combinations of heterotrimeric G proteins composed of Gα, Gβ, and Gγ subunits …
diverse combinations of heterotrimeric G proteins composed of Gα, Gβ, and Gγ subunits …
[HTML][HTML] Rules and mechanisms governing G protein coupling selectivity of GPCRs
G protein-coupled receptors (GPCRs) convert extracellular stimuli into intracellular signaling
by coupling to heterotrimeric G proteins of four classes: G i/o, G q, G s, and G 12/13 …
by coupling to heterotrimeric G proteins of four classes: G i/o, G q, G s, and G 12/13 …
A molecular mechanism to diversify Ca2+ signaling downstream of Gs protein-coupled receptors
J Brands, S Bravo, L Jürgenliemke, L Grätz… - Nature …, 2024 - nature.com
A long-held tenet in inositol-lipid signaling is that cleavage of membrane phosphoinositides
by phospholipase Cβ (PLCβ) isozymes to increase cytosolic Ca2+ in living cells is exclusive …
by phospholipase Cβ (PLCβ) isozymes to increase cytosolic Ca2+ in living cells is exclusive …
Direct interrogation of context-dependent GPCR activity with a universal biosensor platform
G protein-coupled receptors (GPCRs) are the largest family of druggable proteins encoded
in the human genome, but progress in understanding and targeting them is hindered by the …
in the human genome, but progress in understanding and targeting them is hindered by the …
Spatiotemporal GPCR signaling illuminated by genetically encoded fluorescent biosensors
C Kayser, B Melkes, C Derieux, A Bock - Current opinion in pharmacology, 2023 - Elsevier
G protein-coupled receptors (GPCRs) are ligand-activated cell membrane proteins and
represent the most important class of drug targets. GPCRs adopt several active …
represent the most important class of drug targets. GPCRs adopt several active …
Endomembrane-based signaling by GPCRs and G-proteins
F Liccardo, A Luini, R Di Martino - Cells, 2022 - mdpi.com
G-protein-coupled receptors (GPCRs) and G-proteins have a range of roles in many
physiological and pathological processes and are among the most studied signaling …
physiological and pathological processes and are among the most studied signaling …