Results 141 to 150 of about 31,759 (252)

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

British Journal of Pharmacology, Volume 183, Issue 20, Page 6132-6153, October 2026.
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

Arrestin interactions with the μ-opioid receptor

, 2012
Upon agonist binding the u-opioid receptor (MOPr) is phosphorylated and can recruit arrestin-2 (beta-arrestin-l) and arrestin-3 (p-arrestin-2). Apart from promoting the desensitization and intemalization of the MOPr, the binding of arrestins can also ...
Saxena, Kunal
core  

Predictors of in vitro response to somatostatin and dopamine receptor‐targeted treatments are lacking in clinically non‐functioning pituitary tumors

Journal of Neuroendocrinology, Volume 38, Issue 10, October 2026.
Abstract Clinically non‐functioning pituitary neuroendocrine tumors (NF‐PitNETs) lack effective medical therapies, and the role of somatostatin receptor ligands (SRLs) and dopamine agonists (DAs) in this setting is controversial. We evaluated the in vitro response of NF‐PitNETs to multiple SRL and/or DA treatments, focusing on the role of receptor ...
Claudia Campana, Jessica Amarù, Diego Criminelli Rossi, Anna Arecco, Paolo Nozza, Mara Boschetti, Gianluigi Zona, Diego Ferone, Marica Arvigo, Federico Gatto   +9 more
wiley   +1 more source

Annexin A4 Deficient Ventricular Myocytes Display Advanced Hypertrophy and Electrical Remodeling With Chronic β‐Adrenoceptor Stimulation

The FASEB Journal, Volume 40, Issue 17, 15 September 2026.
Annexin A4 (A4) inhibits adenylyl cyclase 5 and may protect the heart during chronic β‐adrenergic stress. After 7 days of isoprenaline, A4‐deficient mice showed greater cardiomyocyte hypertrophy, prolonged action potentials, reduced Ito, preserved ICaL with altered activation, increased NCX1, and enhanced acute cAMP responsiveness compared with wild ...
Florentina Pluteanu, Alexander Heinick, Manuel Domnik‐Lehnert, Frank U. Müller, Christina Hermes   +4 more
wiley   +1 more source

β‑Arrestin‑2 BRET Biosensors Detect Different β‑Arrestin‑2 Conformations in Interaction with GPCRs

, 2019
β-Arrestins are critical regulators of G protein-coupled receptors (GPCRs) that desensitize G protein signaling, promote receptor internalization, and initiate signaling on their own.
Ralf Jockers, Julie Dam, Julie Dam (8208489), Ralf Jockers (245630), Atsuro Oishi, Atsuro Oishi (8208486)   +5 more
core   +1 more source

Structure and Self-Association of Arrestin-1

Arrestins halt cell signaling by binding to phosphorylated activated G protein-coupled receptors. Arrestin-1 binds to rhodopsin, arrestin-4 binds to cone opsins, and arrestins-2,3 bind to the rest of GPCRs. In addition, it has been reported that arrestin-
Salom, David, Palczewski, Krzysztof
core   +1 more source

Editorial: Atypical Functions of Leukocyte Chemoattractant Receptors

Frontiers in Immunology, 2020
José Luis Rodríguez-Fernández, Mario Mellado, Marcus Thelen, Philip M. Murphy   +3 more
doaj   +1 more source

Molecular mechanism of β-arrestin 2 interaction with phosphorylated intracellular loop 3 of dopamine receptor D2

Communications Biology
G protein-coupled receptors (GPCRs), the key regulators of cellular signaling, transduce signals through G proteins or arrestins. G protein- or arrestin-mediated signal transduction induces distinct functional consequences, and therefore the molecular ...
Kiae Kim, Jeong Seok Ji, Hee Ryung Kim, Yoonjung Choi, Hyung Ho Lee, Asuka Inoue, Ka Young Chung   +6 more
doaj   +1 more source

Arrestin development: a role for β-arrestins in viral myocarditis

American Journal of Physiology-Heart and Circulatory Physiology
Shaoni Dasgupta, Thomas Dempster, Kristine Y. DeLeon-Pennell   +2 more
openaire   +2 more sources

Arrestins as programmable integrators of GPCR signaling: structural microstates, spatiotemporal logic, and therapeutic control. [PDF]

Cell Discov
He Q, Zhao LH, Xu HE.
europepmc   +1 more source