Results 91 to 100 of about 45,700 (234)

A small molecule enhances arrestin-3 binding to the β2-adrenergic receptor

Communications Chemistry
Excessive signaling by various GPCRs underlies a variety of human disorders. Suppression of GPCRs by “enhanced” arrestin mutants was proposed as therapy.
Han Kurt, Ali Akyol, Cagdas Devrim Son, Chen Zheng, Irene Gado, Massimiliano Meli, Erica Elisa Ferrandi, Ivan Bassanini, Francesca Vasile, Vsevolod V. Gurevich, Aylin Nebol, Esra Cagavi, Giulia Morra, Ozge Sensoy   +13 more
doaj   +1 more source

Distinct and shared roles of β-arrestin-1 and β-arrestin-2 on the regulation of C3a receptor signaling in human mast cells. [PDF]

PLoS ONE, 2011
The complement component C3a induces degranulation in human mast cells via the activation of cell surface G protein coupled receptors (GPCR; C3aR).
Arpana Vibhuti, Kshitij Gupta, Hariharan Subramanian, Qiang Guo, Hydar Ali   +4 more
doaj   +1 more source

Endocrinology and the brain: Corticotropin-Releasing Hormone signaling [PDF]

, 2017
Corticotropin-releasing hormone (CRH) is a key player of basal and stress activated responses in the hypothalamic-pituitary-adrenal axis (HPA) and in extrahypothalamic circuits, where it functions as a neuromodulator to orchestrate humoral and behavioral
Armando, Natalia Giannina, Dos Santos Claro, Paula Ayelen, Inda, María Carolina, Silberstein Cuña, Susana Iris   +3 more
core   +2 more sources

Are we hallucinating or can psychedelic drugs modulate the immune system to control inflammation?

British Journal of Pharmacology, EarlyView.
Psychedelic drugs that activate 5‐HT2A receptors have been long used for cultural, medicinal and recreational purposes. Interest in psychedelics for treating psychiatric disorders has resurged recently and is well documented; less well recognised are their anti‐inflammatory properties. Growing evidence now demonstrates that psychedelics modulate immune
Omar Qureshi, Jamie Cowley, Ashley Pegg, Alison J. Cooper, John Gordon, Catherine A. Brady, Antonio Belli, Sam Butterworth, Rachel Upthegrove, Nick Andrews, Nicholas M. Barnes   +10 more
wiley   +1 more source

ATHENA: A Phase 3, Open-Label Study Of The Safety And Effectiveness Of Oliceridine (TRV130), A G-Protein Selective Agonist At The µ-Opioid Receptor, In Patients With Moderate To Severe Acute Pain Requiring Parenteral Opioid Therapy. [PDF]

, 2019
Background:Pain management with conventional opioids can be challenging due to dose-limiting adverse events (AEs), some of which may be related to the simultaneous activation of β-arrestin (a signaling pathway associated with opioid-related AEs) and G ...
Beard, Timothy L, Bergese, Sergio D, Berkowitz, Richard D, Brzezinski, Marek, Cochrane, Kristina, Habib, Ashraf S, Hammer, Gregory B, Mace, Sharon E, Minkowitz, Harold S, Pan, Peter H, Wase, Linda   +10 more
core  

Identification and light-dependent translocation of a cone-specific antigen, cone arrestin, recognized by monoclonal antibody 7G6 [PDF]

, 2003
PURPOSE: To elucidate the antigen recognized by monoclonal antibody (mAb) 7G6, a widely used cone-specific marker. METHODS: 7G6 immunocytochemistry was performed on sections of human, primate, and bovine retina.
Baehr, Wolfgang, Church-Kopish, Jill, Cuenca, Nicolás, Frederick, Jeanne M., Ivanova, Tamara, MacLeish, Peter R., Zhang, Houbin   +6 more
core   +2 more sources

Compartmentalisation in cAMP signalling: A phase separation perspective

British Journal of Pharmacology, EarlyView.
Cells rely on precise spatiotemporal control of signalling pathways to ensure functional specificity. The compartmentalisation of cyclic AMP (cAMP) and protein kinase A (PKA) signalling enables distinct cellular responses within a crowded cytoplasmic space.
Milda Folkmanaite, Manuela Zaccolo
wiley   +1 more source

Considering the role of Murine double minute 2 in the cardiovascular system [PDF]

, 2019
The E3 ubiquitin ligase Murine double minute 2 (MDM2) is the main negative regulator of the tumor protein p53 (TP53). Extensive studies over more than two decades have confirmed MDM2 oncogenic role through mechanisms both TP53-dependent and TP53 ...
Lam, Brian, Roudier, Emile
core   +1 more source

The potential for biased signalling in the P2Y receptor family of GPCRs

British Journal of Pharmacology, EarlyView.
The purinergic receptor family is primarily activated by nucleotides, and contains members of both the G protein coupled‐receptor (GPCR) superfamily (P1 and P2Y) and ligand‐gated ion channels (P2X). The P2Y receptors are widely expressed in the human body, and given the ubiquitous nature of nucleotides, purinergic signalling is involved with a plethora
Claudia M. Sisk, Simon Pitchford, Graham Ladds   +2 more
wiley   +1 more source

A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice. [PDF]

, 2014
It is well known that the ω-3 fatty acids (ω-3-FAs; also known as n-3 fatty acids) can exert potent anti-inflammatory effects. Commonly consumed as fish products, dietary supplements and pharmaceuticals, ω-3-FAs have a number of health benefits ascribed ...
Akiyama, Taro E, Armando, Aaron M, Bogner-Strauss, Juliane G, Chi, Tyler J, Chung, Heekyung, Cox, Jason M, Di Salvo, Jerry, Evans, Ronald M, Hah, Nasun, Lackey, Denise, Lagakos, William S, McNelis, Joanne, Oh, Da Young, Olefsky, Jerrold M, Pessentheiner, Ariane R, Powels, Mary Ann, Quehenberger, Oswald, Sasik, Roman, Sinz, Christopher, Walenta, Evelyn, Watkins, Steven M   +20 more
core   +1 more source