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 …

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 …

GLP-1R signaling neighborhoods associate with the susceptibility to adverse drug reactions of incretin mimetics

SC Wright, A Motso, S Koutsilieri, CM Beusch… - Nature …, 2023 - nature.com
G protein-coupled receptors are important drug targets that engage and activate signaling
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 …

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 …

[HTML][HTML] Rules and mechanisms governing G protein coupling selectivity of GPCRs

I Masuho, R Kise, P Gainza, E Von Moo, X Li, R Tany… - Cell reports, 2023 - cell.com
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 …

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 …

Direct interrogation of context-dependent GPCR activity with a universal biosensor platform

R Janicot, M Maziarz, JC Park, J Zhao, A Luebbers… - Cell, 2024 - cell.com
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 …

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 …

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 …