β− Arrestins: structure, function, physiology, and pharmacological perspectives

J Wess, AB Oteng, O Rivera-Gonzalez… - Pharmacological …, 2023 - ASPET
The two β-arrestins, β-arrestin-1 and-2 (systematic names: arrestin-2 and-3, respectively),
are multifunctional intracellular proteins that regulate the activity of a very large number of …

[HTML][HTML] G protein-coupled receptors in neurodegenerative diseases and psychiatric disorders

TS Wong, G Li, S Li, W Gao, G Chen, S Gan… - … and Targeted Therapy, 2023 - nature.com
Neuropsychiatric disorders are multifactorial disorders with diverse aetiological factors.
Identifying treatment targets is challenging because the diseases are resulting from …

Phosphorylation barcodes direct biased chemokine signaling at CXCR3

DS Eiger, JS Smith, T Shi, TM Stepniewski, CF Tsai… - Cell chemical …, 2023 - cell.com
G protein-coupled receptor (GPCR)-biased agonism, selective activation of certain signaling
pathways relative to others, is thought to be directed by differential GPCR phosphorylation" …

G protein–biased GPR3 signaling ameliorates amyloid pathology in a preclinical Alzheimer's disease mouse model

Y Huang, T Rafael Guimarães… - Proceedings of the …, 2022 - National Acad Sciences
Biased G protein–coupled receptor (GPCR) ligands, which preferentially activate G protein
or β-arrestin signaling pathways, are leading to the development of drugs with superior …

[HTML][HTML] GPCRs in intracellular compartments: New targets for drug discovery

I Fasciani, M Carli, F Petragnano, F Colaianni, G Aloisi… - Biomolecules, 2022 - mdpi.com
The architecture of eukaryotic cells is defined by extensive membrane-delimited
compartments, which entails separate metabolic processes that would otherwise interfere …

[HTML][HTML] Targeting the Actions of Muscarinic Receptors on Dopamine Systems: New Strategies for Treating Neuropsychiatric Disorders

EJ Nunes, NA Addy, PJ Conn… - Annual Review of …, 2024 - annualreviews.org
Cholinergic regulation of dopamine (DA) signaling has significant implications for numerous
disorders, including schizophrenia, substance use disorders, and mood-related disorders …

The M1 muscarinic receptor is present in situ as a ligand-regulated mixture of monomers and oligomeric complexes

S Marsango, L Jenkins, JD Pediani… - Proceedings of the …, 2022 - National Acad Sciences
The quaternary organization of rhodopsin-like G protein-coupled receptors in native tissues
is unknown. To address this we generated mice in which the M1 muscarinic acetylcholine …

[HTML][HTML] Cholinergic signaling via muscarinic M1 receptor confers resistance to docetaxel in prostate cancer

J Wang, J Wei, T Pu, A Zeng, V Karthikeyan… - Cell Reports …, 2024 - cell.com
Docetaxel is the most commonly used chemotherapy for advanced prostate cancer (PC),
including castration-resistant disease (CRPC), but the eventual development of docetaxel …

ERNEST COST action overview on the (patho) physiology of GPCRs and orphan GPCRs in the nervous system

N Birgül Iyison, C Abboud, D Abboud… - British Journal of …, 2024 - Wiley Online Library
G protein‐coupled receptors (GPCRs) are a large family of cell surface receptors that play a
critical role in nervous system function by transmitting signals between cells and their …

Alzheimer's disease and clinical trials

D Paul, R Agrawal, S Singh - … of Basic and Clinical Physiology and …, 2024 - degruyter.com
Alzheimer's disease (AD) is spreading its root disproportionately among the worldwide
population. Many genes have been identified as the hallmarks of AD. Based upon the …