Results 81 to 90 of about 7,477 (214)

A Brief History of the β-Arrestins [PDF]

, 2019
Arrestins have now been implicated in the actions of virtually every G protein-coupled receptor (GPCR) for which they have been examined. Originally discovered for their role in the turnoff of visual perception, their newly discovered pleotropic functions in the cellular and physiological actions of GPCRs not only illuminate new mechanisms of signal ...
Marc G, Caron, Lawrence S, Barak
openaire   +2 more sources

Peripheral targets for neuropathic pain

British Journal of Pharmacology, EarlyView.
Neuropathic pain represents a significant clinical challenge, with still limited pharmacological approaches to symptomatic relief. This review focuses on molecular targets implicated in neuropathic pain, particularly those involved in peripheral mechanisms. Using the IUPHAR/BPS database of biological targets, their occurrence together with ‘neuropathic
Amirhossein Afsharipour, Cosmin I. Ciotu, Felix J. Resch, Michael J. M. Fischer   +3 more
wiley   +1 more source

Regulation of cardiac fibroblast-mediated maladaptive ventricular remodeling by β-arrestins.

PLoS ONE, 2019
Cardiac fibroblasts (CF) play a critical role in post-infarction remodeling which can ultimately lead to pathological fibrosis and heart failure.
Jennifer L Philip, Xianyao Xu, Mei Han, Shahab A Akhter, Md Abdur Razzaque   +4 more
doaj   +1 more source

Cannabinoid CB1 allosteric ligands suppress inflammatory pain in male mice without tolerance, motor impairment, memory deficits or respiratory depression

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Positive allosteric modulators (PAMs) engage sites distinct from the orthosteric CB1 cannabinoid receptor binding site. GAT211, a racemic ligand, contains GAT228 (R) and GAT229 (S) enantiomers. Whether enantiomer‐mediated differences in allosteric activation or positive allosteric modulation translate into differences in
Ifeoluwa D. Solomon, Sumanta Garai, Ganesh A. Thakur, Andrea G. Hohmann   +3 more
wiley   +1 more source

SNX9 family mediates βarrestin-independent GPCR endocytosis

Communications Biology
Agonist-stimulated GPCR endocytosis typically occurs via the multi-faceted adaptor proteins known as βarrestins. However, endocytosis of several GPCRs occurs independently of β-arrestins, suggesting an additional mode of GPCR endocytosis, but the ...
Valeria L. Robleto, Ya Zhuo, Joseph M. Crecelius, Sara Benzow, Adriano Marchese   +4 more
doaj   +1 more source

Systematic profiling reveals broad G protein coupling and context‐dependent modulation of cyclic AMP by the orphan receptor GPR139

British Journal of Pharmacology, EarlyView.
Background and Purpose G protein‐coupled receptors (GPCRs) are major drug targets, yet many orphan receptors remain poorly characterized. GPR139 has been implicated in CNS disorders, including schizophrenia and depression, but its signalling mechanisms remain unclear.
Boris Trapkov, Hans Bräuner, Alexander Sebastian Hauser   +2 more
wiley   +1 more source

The c‐Src inhibitor eCF506 diminishes opioid tolerance and reduces β‐arrestin2 recruitment

British Journal of Pharmacology, EarlyView.
Morphine activation of μ receptors causes tolerance through c‐Src activation and β‐arrestin2 recruitment. c‐Src inhibition or degradation reduces β‐arrestin2 recruitment, μ receptor endocytosis, while causing receptor upregulation, all likely contributing to reduced morphine tolerance.
Samuel Singleton, Fraser Nunn, Erika Lace, Álvaro Lorente‐Macías, Rachel Toth, Asier Unciti‐Broceta, Tim G. Hales   +6 more
wiley   +1 more source

Innovations in Obesity Treatment: Beyond Adipose Tissue Dysfunction

Obesity Reviews, EarlyView.
Obesity drives chronic inflammation, insulin resistance, type 2 diabetes, and cancer development through adipocyte dysfunction. Addressing this multisystemic disorder requires integrated strategies beyond diet and exercise, such as thermogenesis activation via menthol or capsinoids and appetite control through GLP‐1/GIP agonists and neuromodulation to ...
Jesica Martínez‐Godfrey, Irene Pomares‐Bri, Paula de Juan‐Maciá, Mariló Olivares‐Vicente, Enrique Barrajón‐Catalán, Vicente Micol, Enrique Roche, María Herranz‐López   +7 more
wiley   +1 more source

The Significance of cGAS‐STING Signaling in Response to Oncogenic Viruses

Cell Biochemistry and Function, Volume 44, Issue 9, September 2026.
ABSTRACT The cyclic GMP‐AMP synthase (cGAS)‐stimulator of interferon genes (STING) signaling pathway, as a key DNA sensor, plays a significant role in the regulation of innate immune responses. This pathway can be activated by sensing abnormal DNA, and is of great significance for resisting the invasion of pathogenic microorganisms and maintaining ...
Limei Guo, Li Li, Fang Wang, Wen Liu, Yan Zhang   +4 more
wiley   +1 more source

Sex and Chronic Stress Alter the Distribution of Corticotropin‐Releasing Factor Receptor in Rat Hippocampus Following Oxycodone Conditioned Place Preference

Synapse, Volume 80, Issue 5, September 2026.
Chronic stress modifies the effect of oxycodone conditioned place preference (Oxy CPP) on corticotropin releasing factor 1 (CRFR1) subcellular distributions in hippocampal subregions. These stress‐ and oxycodone‐induced changes in CRFR1 density may influence sex differences in hippocampal learning and memory processes both at baseline and following Oxy
Dana N. Silberstein, Zoha Baig, Batsheva Rubin, Fangmin Yu, Joshua Kogan, Jason D. Gray, Yan Zhou, Teresa A. Milner   +7 more
wiley   +1 more source