Cannabinoid 1 (CB1) receptor arrestin subtype‐selectivity and phosphorylation dependence

JJ Manning, G Rawcliffe, DB Finlay… - British journal of …, 2023‏ - Wiley Online Library
Background and purpose Arrestin or G protein bias may be desirable for novel cannabinoid
therapeutics. Arrestin‐2 and arrestin‐3 translocation to CB1 receptor have been suggested …

A multi-dimensional view of context-dependent G protein-coupled receptor function

M Marti-Solano - Biochemical Society Transactions, 2023‏ - portlandpress.com
G protein-coupled receptor (GPCR) family members can sense an extraordinary variety of
biomolecules to activate intracellular signalling cascades that modulate key aspects of cell …

Human pluripotent stem cells as a translational toolkit in psychedelic research in vitro

JA Salerno, S Rehen - Iscience, 2024‏ - cell.com
Psychedelics, recognized for their impact on perception, are resurging as promising
treatments with rapid onset for mood and substance use disorders. Despite increasing …

Kinetic analysis of endogenous β2‐adrenoceptor‐mediated cAMP GloSensor™ responses in HEK293 cells

SA Cullum, DB Veprintsev… - British Journal of …, 2023‏ - Wiley Online Library
Abstract Background and Aim Standard pharmacological analysis of agonist activity utilises
measurements of receptor‐mediated responses at a set time‐point, or at the peak response …

Investigation of adenosine A1 receptor-mediated β-arrestin 2 recruitment using a split-luciferase assay

L Saecker, H Häberlein, S Franken - Frontiers in Pharmacology, 2023‏ - frontiersin.org
Background: Adenosine A1 receptor (A1AR) plays a prominent role in neurological and
cardiac diseases and inflammatory processes. Its endogenous ligand adenosine is known to …

[HTML][HTML] GPCR kinase subtype requirements for arrestin-2 and-3 translocation to the cannabinoid CB1 receptor and the consequences on G protein signalling

JJ Manning, DB Finlay, M Glass - Biochemical pharmacology, 2024‏ - Elsevier
Arrestins are key negative regulators of G Protein-Coupled Receptors (GPCRs) through
mediation of G protein desensitisation and receptor internalisation. Arrestins can also …

Genetic analysis and clinical features of three Chinese patients with Oguchi disease

X Wei, H Li, S Wu, T Zhu, R Sui - Documenta Ophthalmologica, 2023‏ - Springer
Background Oguchi disease is a rare autosomal recessive form of congenital stationary
night blindness caused by disease-causing variants in the rhodopsin kinase gene (GRK1) or …

ClickArr: A novel, high-throughput assay for evaluating β-arrestin isoform recruitment

AR French, YJ Meqbil, RM van Rijn - Frontiers in Pharmacology, 2023‏ - frontiersin.org
Background: Modern methods for quantifying signaling bias at G protein–coupled receptors
(GPCRs) rely on using a single β-arrestin isoform. However, it is increasingly appreciated …

Characterization of adenylyl cyclase isoform 6 residues interacting with forskolin

V Bhatia, S Maghsoudi, M Hinton, AY Bhagirath… - Biology, 2023‏ - mdpi.com
Simple Summary Adenylyl cyclase isoform 6 is the only member of the adenylyl cyclase
enzyme family to be inhibited by low oxygen levels. We studied the unique structure of the …

Deciphering downstream receptor signaling

M Filizola, JA Javitch - Science, 2023‏ - science.org
G protein–coupled receptors (GPCRs) are important cell-surface signaling proteins that are
responsive to diverse extracellular stimuli and are key drug targets. Understanding how …