Results 1 to 10 of about 11,411 (182)
Highly biased agonism for GPCR ligands via nanobody tethering. [PDF]
Nat Commun, 2023 Ligand-induced activation of G protein-coupled receptors (GPCRs) can initiate signaling through multiple distinct pathways with differing biological and physiological outcomes.
Sachdev S +3 more
europepmc +5 more sources
A structural mechanism of nuclear receptor biased agonism. [PDF]
Proc Natl Acad Sci U S A, 2022 Efforts to decrease the adverse effects of nuclear receptor (NR) drugs have yielded experimental agonists that produce better outcomes in mice. Some of these agonists have been shown to cause different, not just less intense, on-target transcriptomic effects; however, a structural explanation for such agonist-specific effects remains unknown.
Nemetchek MD +4 more
europepmc +5 more sources
Biased agonism: the quest for the analgesic holy grail. [PDF]
Pain Rep, 2018 . Opioids alleviate pain, but adverse effects severely limit their usefulness. To solve this problem, biased ligands favoring 1 signaling pathway downstream of the μ-opioid receptor over another are being developed.
Stanczyk MA, Kandasamy R.
europepmc +4 more sources
Biased agonism at chemokine receptors. [PDF]
Cell Signal, 2021 In the human chemokine system, interactions between the approximately 50 known endogenous chemokine ligands and 20 known chemokine receptors (CKRs) regulate a wide range of cellular functions and biological processes including immune cell activation and homeostasis, development, angiogenesis, and neuromodulation.
Eiger DS +4 more
europepmc +4 more sources
Modelling G protein-biased agonism using GLP-1 receptor C-terminal mutations. [PDF]
Mol MetabBackground and aim: The glucagon-like peptide-1 receptor (GLP-1R) is a major therapeutic target for type 2 diabetes and obesity. Agonists showing bias in favour of G protein signalling over β-arrestin recruitment and GLP-1R internalisation, e.g ...
Tran HD +5 more
europepmc +2 more sources
Biased receptor functionality versus biased agonism in G-protein-coupled receptors [PDF]
Biomolecular Concepts, 2018 Functional selectivity is a property of G-protein-coupled receptors (GPCRs) by which activation by different agonists leads to different signal transduction mechanisms.
Franco Rafael +5 more
doaj +5 more sources
Biased agonism of GLP-1R and GIPR enhances glucose lowering and weight loss, with dual GLP-1R/GIPR biased agonism yielding greater efficacy. [PDF]
Cell Rep MedSummary: Glucagon-like peptide-1 receptor (GLP-1R) and glucose-dependent insulinotropic polypeptide receptor (GIPR) agonists have recently been shown to play a significant role in the treatment of diabetes and obesity.
Rodriguez R +17 more
europepmc +2 more sources
Biased agonism at β-adrenergic receptors. [PDF]
Cell Signal, 2021 The β-adrenergic receptors (βARs) include three subtypes, β1, β2 and β3. These receptors are widely expressed and regulate numerous physiological processes including cardiovascular and metabolic functions and airway tone. The βARs are also important targets in the treatment of many diseases including hypertension, heart failure and asthma.
Ippolito M, Benovic JL.
europepmc +3 more sources
The therapeutic potential of GLP-1 receptor biased agonism. [PDF]
Br J Pharmacol, 2022 Glucagon‐like peptide‐1 (GLP‐1) receptor agonists are effective treatments for type 2 diabetes as they stimulate insulin release and promote weight loss through appetite suppression. Their main side effect is nausea. All approved GLP‐1 agonists are full agonists across multiple signalling pathways.
Jones B.
europepmc +5 more sources
The β-blocker Nebivolol Is a GRK/β-arrestin Biased Agonist [PDF]
PLoS ONE, 2013 Nebivolol, a third generation β-adrenoceptor (β-AR) antagonist (β-blocker), causes vasodilation by inducing nitric oxide (NO) production. The mechanism via which nebivolol induces NO production remains unknown, resulting in the genesis of much of the ...
Andresen, Bradley T. +9 more
core +8 more sources