Results 91 to 100 of about 29,855 (176)

Signal Transduction and Pathogenic Modifications at the Melanocortin-4 Receptor: A Structural Perspective [PDF]

, 2019
The melanocortin-4 receptor (MC4R) can be endogenously activated by binding of melanocyte-stimulating hormones (MSH), which mediates anorexigenic effects. In contrast, the agouti-related peptide (AgRP) acts as an endogenous inverse agonist and suppresses
Biebermann, Heike, Cerdá-Reverter, José Miguel, Heyder, Nicolas, Kleinau, Gunnar, Krude, Heiko, Kwiatkowski, Dennis, Kühnen, Peter, Scheerer, Patrick, Soletto, Lucia, Speck, David, Szczepek, Michal   +10 more
core   +1 more source

Profiling of HCAR1 signalling reveals Gαi/o and Gαs activation without β‐arrestin recruitment and the discovery of an allosteric agonist

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Lactate, historically viewed as a metabolic by‐product, has emerged as a signalling molecule via the G protein–coupled receptor Hydroxycarboxylic Acid Receptor 1 (HCAR1). The receptor is primarily expressed in adipocytes but also found in various other tissues.
Simon Lind, Shane C. Wright, Emilia Gvozdenovic, Kristina Nilsson, Kenneth L. Granberg, Michel Bouvier, Linda C. Johansson   +6 more
wiley   +1 more source

The relationship between the cannabinoids and cardiac remodelling: A comprehensive review of pivotal mechanisms and emerging evidence

British Journal of Pharmacology, EarlyView.
Cardiac remodelling and fibrosis after myocardial infarction or during chronic diseases, such as arterial and pulmonary hypertension or diabetes mellitus, continue to be the more important prognostic factors in determining survival, and so the search for effective anti‐fibrotic interventions is an important target for research and therapy in cardiology.
Anna Krzyżewska, Marta Baranowska‐Kuczko, Hanna Kozłowska   +2 more
wiley   +1 more source

Phosducin regulates the expression of transducin betagamma subunits in rod photoreceptors and does not contribute to phototransduction adaptation. [PDF]

, 2007
For over a decade, phosducin's interaction with the betagamma subunits of the G protein, transducin, has been thought to contribute to light adaptation by dynamically controlling the amount of transducin heterotrimer available for activation by ...
Arshavsky, Vadim Y, Burns, Marie E, Chen, Yen-Ming, Herrmann, Rolf, Krispel, Claudia M, Sokolov, Maxim, Song, Hongman   +6 more
core  

Differential β-arrestin2 requirements for constitutive and agonist-induced internalization of the CB1 cannabinoid receptor [PDF]

, 2013
CB1 cannabinoid receptor (CB1R) undergoes both constitutive and agonist-induced internalization, but the underlying mechanisms of these processes and the role of beta-arrestins in the regulation of CB1R function are not completely understood.
Ahn, Bakshi, Bari, Brailoiu, Coutts, Daigle, Daigle, Dale, Derkinderen, DeWire, Eszter Boros, Fan, Ferguson, Ferguson, Freund, Gaborik, Graham, Guan, Gyombolai, Gábor Turu, Holliday, Hsieh, Hunyady, Jin, Keren, Kleyer, Kouznetsova, Krupnick, Leterrier, Leterrier, László Hunyady, Marullo, McDonald, McDonald, Nguyen, Oakley, Oakley, Pacher, Paing, Parent, Pál Gyombolai, Rinaldi-Carmona, Roche, Rozenfeld, Rozenfeld, Sanchez, Shenoy, Singh, Szekeres, Tohgo, Toth, Turu, Turu, Turu, Turu, Valjent, Varnai, Vines, Ward, Ward, Wei, Woo, Wu, Zhang, Zhao   +64 more
core   +1 more source

Comprehensive transduceromic profiling of NOP receptor ligands at different Gα subunits

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose The nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) is an opioid receptor family member with distinct pharmacology and broad therapeutic potential. NOP receptors regulate functions such as nociception, stress reactivity, reward, mood, autonomic tone, immunity and sleep/wake cycle.
Davide Malfacini, Riccardo Camilotto, Michele Maritan, Erika Morrone, Stephen Afriyie Boateng, Anna Vacilotto, Salvatore Pacifico, Remo Guerrini, Nurulain T. Zaveri, Girolamo Calo'   +9 more
wiley   +1 more source

A new inhibitor of the β-arrestin/AP2 endocytic complex reveals interplay between GPCR internalization and signalling

Nature Communications, 2017
Beta-arrestins play central roles in the mechanisms regulating GPCR signalling and trafficking. Here the authors identify a selective inhibitor of the interaction between β-arrestin and the β2-adaptin subunit of the clathrin adaptor protein AP-2, which ...
Alexandre Beautrait, Justine S. Paradis, Brandon Zimmerman, Jenna Giubilaro, Ljiljana Nikolajev, Sylvain Armando, Hiroyuki Kobayashi, Lama Yamani, Yoon Namkung, Franziska M. Heydenreich, Etienne Khoury, Martin Audet, Philippe P. Roux, Dmitry B. Veprintsev, Stéphane A. Laporte, Michel Bouvier   +15 more
doaj   +1 more source

Phosphorylation-induced conformation of beta(2)-adrenoceptor related to arrestin recruitment revealed by NMR [PDF]

, 2018
The C-terminal region of G-protein-coupled receptors (GPCRs), stimulated by agonist binding, is phosphorylated by GPCR kinases, and the phosphorylated GPCRs bind to arrestin, leading to the cellular responses.
Imai, Shunsuke, Iwai, Hideo, Kofuku, Yutaka, Mizukoshi, Toshimi, Nakata, Kunio, Natsume, Mei, Shimada, Ichio, Shiraishi, Yutaro, Ueda, Takumi   +8 more
core   +2 more sources

Lock, relax, load, and shoot: a molecular perspective on Nedd4 regulation

The FEBS Journal, EarlyView.
Structural basis of inactive and active states of the Nedd4 HECT E3 ligase subfamily, following a ‘lock, relax, load, and shoot’ mechanism. In the locked, autoinhibited state, intramolecular domain interactions restrain the HECT domain. Relaxation releases these restraints, allowing loading of ubiquitin onto the catalytic cysteine, followed by the ...
Masa Janosev, Tomas Obsil, Veronika Obsilova   +2 more
wiley   +1 more source

PAR1 Agonists Stimulate APC-Like Endothelial Cytoprotection and Confer Resistance to Thromboinflammatory Injury [PDF]

, 2018
Stimulation of protease-activated receptor 1 (PAR1) on endothelium by activated protein C (APC) is protective in several animal models of disease, and APC has been used clinically in severe sepsis and wound healing.
Aisiku, Omozuanvbo, Ceunynck, Karen De, Chaudhry, Sharjeel A., Dockendorff, Chris, Fitch-Tewfik, Jennifer L., Flaumenhaft, Robert, Higgins, Sarah J., Ingber, Donald E., Jain, Abhishek, Parikh, Samir M., Peters, Christian G.   +10 more
core   +1 more source