Results 21 to 30 of about 11,641 (225)
G Protein-coupled Receptor Biased Agonism. [PDF]
J Cardiovasc Pharmacol, 2016 G protein-coupled receptors are the largest family of targets for current therapeutics. The classic model of their activation was binary, where agonist binding induced an active conformation and subsequent downstream signaling. Subsequently, the revised concept of biased agonism emerged, where different ligands at the same G protein-coupled receptor ...
Hodavance SY +3 more
europepmc +4 more sources
A Non-covalent Ligand Reveals Biased Agonism of the TRPA1 Ion Channel [PDF]
Neuron, 2021 Simon Vu +2 more
exaly +2 more sources
Structural determinants of 5-HT2B 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 +10 more
europepmc +4 more sources
Structural and Functional Basis for Biased Agonism at the 5-hydroxytryptamine 5A Receptor [PDF]
Molecular BiomedicineXiaoyu Zhang +9 more
doaj +2 more sources
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 +10 more
doaj +1 more source
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 +15 more
doaj +1 more source
Influence of Chemokine N-Terminal Modification on Biased Agonism at the Chemokine Receptor CCR1 [PDF]
International Journal of Molecular Sciences, 2019 Julie Sanchez +2 more
exaly +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 +2 more
openaire +2 more sources
Hepatology, EarlyView., 2022 CHIN117 is a dual cysteinyl leukotriene receptor 1 (CYSLTR1) antagonist and G‐protein‐coupled bile acid receptor 1 (GPBAR1) agonist. In the liver, GPBAR1 and CYSLTR1 are coexpressed by liver sinusoidal endothelial cells (LSECs), HSCs, circulating monocytes/macrophages, and liver resident macrophages (Kupffer cells).
Michele Biagioli +13 more
wiley +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 +3 more
openaire +2 more sources