Results 21 to 30 of about 11,411 (182)

The Old and New Visions of Biased Agonism Through the Prism of Adenosine Receptor Signaling and Receptor/Receptor and Receptor/Protein Interactions. [PDF]

Front Pharmacol, 2020
Biased signaling is a concept that has arisen in the G protein-coupled receptor (GCPR) research field, and holds promise for the development of new drug development strategies.
Franco R, Rivas-Santisteban R, Reyes-Resina I, Navarro G.   +3 more
europepmc   +2 more sources

Exploring Biased Agonism at FPR1 as a Means to Encode Danger Sensing. [PDF]

Cells, 2020
Ligand-based selectivity in signal transduction (biased signaling) is an emerging field of G protein-coupled receptor (GPCR) research and might allow the development of drugs with targeted activation profiles.
Gröper J, König GM, Kostenis E, Gerke V, Raabe CA, Rescher U.   +5 more
europepmc   +2 more sources

Structural determinants of 5-HT_2B receptor activation and biased agonism. [PDF]

Nat Struct Mol Biol, 2018
Serotonin (5-hydroxytryptamine; 5-HT) receptors modulate a variety of physiological processes ranging from perception, cognition and emotion to vascular and smooth muscle contraction, platelet aggregation, gastrointestinal function and reproduction.
McCorvy JD, Wacker D, Wang S, Agegnehu B, Liu J, Lansu K, Tribo AR, Olsen RHJ, Che T, Jin J, Roth BL.   +10 more
europepmc   +4 more sources

A Non-covalent Ligand Reveals Biased Agonism of the TRPA1 Ion Channel. [PDF]

Neuron, 2021
Liu C, Reese R, Vu S, Rougé L, Shields SD, Kakiuchi-Kiyota S, Chen H, Johnson K, Shi YP, Chernov-Rogan T, Greiner DMZ, Kohli PB, Hackos D, Brillantes B, Tam C, Li T, Wang J, Safina B, Magnuson S, Volgraf M, Payandeh J, Zheng J, Rohou A, Chen J.   +23 more
europepmc   +2 more sources

Biased action of the CXCR4-targeting drug plerixafor is essential for its superior hematopoietic stem cell mobilization

Communications Biology, 2021
Jørgensen et al. investigate the effects of the CXCR4 targeting agents, AMD3100 (Plerixafor) and AMD11070, and show that AMD3100, unlike AMD11070, is biased with intrinsic β-arrestin recruitment agonism and full G protein antagonism. They finally propose
Astrid S. Jørgensen, Viktorija Daugvilaite, Katia De Filippo, Christian Berg, Masa Mavri, Tau Benned-Jensen, Goda Juzenaite, Gertrud Hjortø, Sara Rankin, Jon Våbenø, Mette M. Rosenkilde   +10 more
doaj   +1 more source

Partial agonism improves the anti-hyperglycaemic efficacy of an oxyntomodulin-derived GLP-1R/GCGR co-agonist

Molecular Metabolism, 2021
Objective: Glucagon-like peptide-1 and glucagon receptor (GLP-1R/GCGR) co-agonism can maximise weight loss and improve glycaemic control in type 2 diabetes and obesity.
Phil Pickford, Maria Lucey, Roxana-Maria Rujan, Emma Rose McGlone, Stavroula Bitsi, Fiona B. Ashford, Ivan R. Corrêa, David J. Hodson, Alejandra Tomas, Giuseppe Deganutti, Christopher A. Reynolds, Bryn M. Owen, Tricia M. Tan, James Minnion, Ben Jones, Stephen R. Bloom   +15 more
doaj   +1 more source

Recent developments in biased agonism [PDF]

Current Opinion in Cell Biology, 2014
The classic paradigm of G protein-coupled receptor (GPCR) activation was based on the understanding that agonist binding to a receptor induces or stabilizes a conformational change to an 'active' conformation. In the past decade, however, it has been appreciated that ligands can induce distinct 'active' receptor conformations with unique downstream ...
James W, Wisler, Kunhong, Xiao, Alex R B, Thomsen, Robert J, Lefkowitz   +3 more
openaire   +2 more sources

Structural and Functional Basis for Biased Agonism at the 5-hydroxytryptamine 5A Receptor. [PDF]

Mol Biomed
Zhang X, Xie L, Chen P, Yu J, Tian X, Wang L, Wei J, Shao Z, Yan W, Xu Z.   +9 more
europepmc   +2 more sources

A Pluridimensional View of Biased Agonism [PDF]

Molecular Pharmacology, 2016
When studying G protein-coupled receptor (GPCR) signaling and ligand-biased agonism, at least three dimensional spaces must be considered, as follows: 1) the distinct conformations that can be stabilized by different ligands promoting the engagement of different signaling effectors and accessory regulators; 2) the distinct subcellular trafficking that ...
Claudio M, Costa-Neto, Lucas T, Parreiras-E-Silva, Michel, Bouvier   +2 more
openaire   +2 more sources

Biased agonism at G protein-coupled receptors

Cellular Signalling, 2021
G protein-coupled receptors (GPCRs) represent the largest family of approved therapeutic targets. Ligands stimulating these receptors specifically activate multiple signalling pathways that induce not only the desired therapeutic response, but sometimes untolerated side effects that limit their clinical use.
Karim, Nagi, Onaran, H. Ongun
openaire   +4 more sources