Results 111 to 120 of about 11,411 (182)

Biased agonism at histamine H1 receptors

, 2018
Fil: Burghi, Valeria. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Investigaciones Farmacológicas. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica.
Burghi, Valeria, Echeverría, Emiliana Beatriz, Díaz Nebreda, Antonela, Zappia, Carlos Daniel, Shayo, Carina Claudia, Davio, Carlos Alberto, Monczor, Federico, Fernandez, Natalia   +7 more
openaire   +1 more source

Global Trends in Oliceridine (TRV130) Research from 2013 to 2024: A Bibliometrics and Knowledge Graph Analysis

Drug Design, Development and Therapy
Cong Wang,1 Lidan Liu,1 Xue Bai2 1Department of Anesthesiology, Shengjing Hospital of China Medical University, Shenyang, Liaoning Province, People’s Republic of China; 2Department of Health Management, Shengjing Hospital of China Medical University ...
Wang C, Liu L, Bai X
doaj  

Functional Selectivity of Cannabinoid Type 1 G Protein-Coupled Receptor Agonists in Transactivating Glycosylated Receptors on Cancer Cells to Induce Epithelial–Mesenchymal Transition Metastatic Phenotype

Cells
Understanding the role of biased G protein-coupled receptor (GPCR) agonism in receptor signaling may provide novel insights into the opposing effects mediated by cannabinoids, particularly in cancer and cancer metastasis.
David A. Bunsick, Jenna Matsukubo, Rashelle Aldbai, Leili Baghaie, Myron R. Szewczuk   +4 more
doaj   +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

Ectopic, hepatic GLP-1R agonism enhances the weight loss efficacy of GLP-1 analogues

Molecular Metabolism
Objectives: Unimolecular triagonists drive substantial weight loss in patients with obesity by engaging the glucagon-like peptide 1 receptor (GLP-1R) and glucose dependent insulinotropic polypeptide receptor (GIPR) to reduce food intake (FI) and the ...
Jonathan D. Douros, Megan Capozzi, Aaron Novikoff, Jacek Mokrosinski, Barent DuBois, Joseph Stock, Rebecca Rohlfs, Mikayla Anderson, Dominika J. Jedrzejcyk, Svend Poulsen, Erik Oude Blenke, Tomas Dago, Kasper Huus, Peder L. Nørby, Sune Kobberup, Marita Rivir, Joyce Sorrell, Stephanie A. Mowery, Daniel J. Drucker, David A. D'Alessio, Jonathan E. Campbell, Timo D. Müller, Diego Perez-Tilve, Brian Finan, Patrick J. Knerr   +24 more
doaj   +1 more source

Structure-Activity Assessment and In-Depth Analysis of Biased Agonism in a Set of Phenylalkylamine 5-HT_2A Receptor Agonists. [PDF]

ACS Chem Neurosci, 2023
Pottie E, Poulie CBM, Simon IA, Harpsøe K, D'Andrea L, Komarov IV, Gloriam DE, Jensen AA, Kristensen JL, Stove CP.   +9 more
europepmc   +1 more source

Control of human pancreatic beta cell kinome by glucagon-like peptide-1 receptor biased agonism. [PDF]

Diabetes Obes Metab, 2023
Xiao J, El Eid L, Buenaventura T, Boutry R, Bonnefond A, Jones B, Rutter GA, Froguel P, Tomas A.   +8 more
europepmc   +1 more source

Biased Agonism or “Biaism” for Dummies: A Commentary

Receptors
That signaling bias is a nth level of complexity in the understanding of G protein-coupled receptor (GPCR) activation is a first fact. That its exhaustive description, including the mode d’emploi of its quantitative measurement, remains a challenge is a second fact.
Jean A. Boutin, Jérôme Leprince
openaire   +1 more source

Spatially diffuse cAMP signalling with oppositely biased GLP-1 receptor agonists in β-cells despite differences in receptor localisation

Molecular Metabolism
Internalisation of G protein-coupled receptors (GPCRs) can contribute to altered cellular responses by directing signalling from non-canonical locations, such as endosomes.
Shiqian Chen, Carolina B. Lobato, Carissa Wong, Yusman Manchanda, Katrina Viloria, Iona Davies, Daniel B. Andersen, Julia Ast, Kyle W. Sloop, David J. Hodson, Johannes Broichhagen, Steve Bloom, Jens J. Holst, Tricia Tan, Alejandra Tomas, Ben Jones   +15 more
doaj   +1 more source

Cellular Electrical Impedance as a Method to Decipher CCR7 Signalling and Biased Agonism. [PDF]

Int J Mol Sci, 2022
Vanalken N, Boon K, Doijen J, Schols D, Van Loy T.   +4 more
europepmc   +1 more source