Results 91 to 100 of about 871,508 (182)

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

Methods to characterize protein interactions with β-arrestin in cellulo: Monitoring partner interactions with β-arrestins

, 2019
International audienceβ-Arrestins 1 and 2 (β-arr1 and β-arr2) are ubiquitous proteins with common and distinct functions. They were initially identified as proteins recruited to stimulated G protein-coupled receptors (GPCRs), regulating their ...
Alexander, Revu,, Isaure Lot, Revu Ann Alexander, Alexander, Revu, Ann, Lot, Isaure, Enslen, Hervé, Hervé Enslen   +6 more
core   +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

Positive modulation of glucagon‐like peptide 1 (GLP‐1) receptor by endogenous haemorphins with implications in glucose metabolism and diabetes

British Journal of Pharmacology, EarlyView.
Haemorphins act on GLP‐1 receptor (GLP‐1R) activity and signalling in a positive allosteric manner. This leads to potentiated GLP‐1‐mediated activity and signalling, as well as insulin synthesis, which may have implications for glucose metabolism and, thereby, diabetes and obesity. (The graph was created in BioRender.com).
Farheen Badrealam Khan, Rwdah Mohamed Alameri, Yasir S. Raouf, Damien Maurel, Naiem Ahmad Wani, Anatoliy Shmygol, Irfa Anwar, Heng B. See, Elizabeth K. M. Johnstone, Elodie Dupuis, Eric Trinquet, Kevin D. G. Pfleger, Emilia Oueis, Mohammed Akli Ayoub   +13 more
wiley   +1 more source

EPHX2 Loss Promotes CRC Migration via EET‐Dependent Chemokine Elevation and Mitochondrial Defect

Cancer Science, EarlyView.
Loss of EPHX2 promotes EET accumulation, which in turn enhances CXCL and ROS production, thereby promoting the migratory and invasive abilities of CRC cells. ABSTRACT Epoxide hydrolase 2 (EPHX2) is a key enzyme in fatty acid metabolism that metabolizes epoxyeicosatrienoic acids (EETs), lipid mediators involved in inflammation, angiogenesis, and ...
Jianjun Zhu, Jingjia Chang, Zhiyong Li, Jin Wu, Pengfei Yu, Jingjing Zheng, Li Li, Jia Tao, Hao Wu, Yintao Li, Ming Liu   +10 more
wiley   +1 more source

Dual Mode of glucagon receptor internalization: Role of PKCα, GRKs and β-arrestins

, 2011
Glucagon levels are elevated in diabetes and some liver diseases. Increased glucagon secretion leads to abnormal stimulation of glucagon receptors (GRs) and consequent elevated glucose production in the liver.
Amy Nguyen, Bouscarel, Bernard, Nguyen, Amy, Ceryak, Susan, Krilov, Lada, Miyazaki, Teruo, Williams, Russell, Unson, Cecilia G., Russell Williams, Norman H. Lee, Cecilia G. Unson, Lee, Norman H., Susan Ceryak, Bernard Bouscarel, Teruo Miyazaki, Lada Krilov   +15 more
core   +1 more source

Imaging Ligand-Dependent Activation of CXCR7

Neoplasia: An International Journal for Oncology Research, 2009
Chemokine CXCL12 is proposed to promote multiple steps in growth of primary tumors and progression to metastatic disease in more than 20 different cancers.
Kathryn E. Luker, Mudit Gupta, Jessica M. Steele, Bradley R. Foerster, Gary D. Luker   +4 more
doaj   +1 more source

Incretin‐Based Therapies as Cardiometabolic Interventions: Outcome Hierarchy, Receptor‐Network Pharmacology and Phenotype‐Based Clinical Positioning

Diabetes, Obesity and Metabolism, EarlyView.
ABSTRACT Aims Incretin‐based pharmacotherapy was initially developed to improve glucose‐dependent insulin secretion and glycaemic control in type 2 diabetes, but its clinical interpretation has expanded substantially with cardiovascular outcome trials, kidney outcome data, obesity studies and next‐generation polyagonist development.
Ferenc Sztanek, Hajnalka Lőrincz, Mariann Harangi, Attila Csaba Nagy   +3 more
wiley   +1 more source

Src and β-arrestins regulate Akt phosphorylation in response to ghrelin in 3T3-L1 preadipocyte cells.

, 2013
A, Effects of the Src inhibitor PP2 and its negative control, PP3, on the ghrelin-induced Akt activation in 3T3-L1 preadipocyte cells. Serum-starved cells were pretreated with PP2 (5 µM, 30 min) or PP3 (5 µM, 30 min) before ghrelin stimulation (100 nM ...
Felipe F. Casanueva (130305), Maria Pardo (374230), Jesus P. Camiña (5653873), Marily Theodoropoulou (374229), Maria Lodeiro (374228)   +4 more
core   +1 more source

Conformational Sensors and Domain Swapping Reveal Structural and Functional Differences between β-Arrestin Isoforms

Cell Reports, 2019
Summary: Desensitization, signaling, and trafficking of G-protein-coupled receptors (GPCRs) are critically regulated by multifunctional adaptor proteins, β-arrestins (βarrs).
Eshan Ghosh, Hemlata Dwivedi, Mithu Baidya, Ashish Srivastava, Punita Kumari, Tomek Stepniewski, Hee Ryung Kim, Mi-Hye Lee, Jaana van Gastel, Madhu Chaturvedi, Debarati Roy, Shubhi Pandey, Jagannath Maharana, Ramon Guixà-González, Louis M. Luttrell, Ka Young Chung, Somnath Dutta, Jana Selent, Arun K. Shukla   +18 more
doaj   +1 more source