Biased agonism of G protein-coupled receptors as a novel strategy for osteoarthritis therapy [PDF]
Bone ResearchOsteoarthritis (OA) is a prevalent degenerative joint disorder marked by chronic pain, inflammation, and cartilage loss, with current treatments limited to symptom relief.
Xiangbo Meng, Ling Qin, Xinluan Wang
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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
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Physiological implications of biased signaling at histamine H2 receptors. [PDF]
Frontiers in Pharmacology, 2015 Histamine mediates numerous functions acting through its four receptor subtypes all belonging to the large family of seven transmembrane G-protein coupled receptors (GPCRs).
Natalia eAlonso +14 more
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Hyperactivity in Mice Induced by Opioid Agonists with Partial Intrinsic Efficacy and Biased Agonism Administered Alone and in Combination with Morphine [PDF]
Biomolecules, 2023 Opioid analgesics such as morphine and fentanyl induce mu-opioid receptor (MOR)-mediated hyperactivity in mice. Herein, we show that morphine, fentanyl, SR-17018, and oliceridine have submaximal intrinsic efficacy in the mouse striatum using 35S-GTPγS ...
Agnes Acevedo-Canabal +7 more
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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 +4 more sources
Structural basis of protease-activated receptor 2 activation and biased agonism [PDF]
Cell DiscoveryProtease-activated receptor 2 (PAR2) is a transmembrane receptor that is irreversibly activated by proteolytic cleavage of its N-terminus via extracellular proteases, resulting in the release of the tethered ligand (TL), which binds to and activates the ...
Xinyan Zhu +5 more
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Highly biased agonism for GPCR ligands via nanobody tethering [PDF]
Nature CommunicationsLigand-induced activation of G protein-coupled receptors (GPCRs) can initiate signaling through multiple distinct pathways with differing biological and physiological outcomes.
Shivani Sachdev +3 more
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Gating Mechanism for Biased Agonism at Angiotensin II Type 1 Receptors [PDF]
MoleculesFor the interaction of angiotensin II (AngII) with AngII type 1 receptors (AT1R), two potential proton hopping pathways have been identified, each associated with distinct physiological outcomes.
Graham J. Moore +5 more
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The Old and New Visions of Biased Agonism Through the Prism of Adenosine Receptor Signaling and Receptor/Receptor and Receptor/Protein Interactions [PDF]
Frontiers in Pharmacology, 2021 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.
Rafael Franco +6 more
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Biased Agonism as a Mechanism for Differential Signaling by Chemokine Receptors [PDF]
Journal of Biological Chemistry, 2013 Chemokines display considerable promiscuity with multiple ligands and receptors shared in common, a phenomenon that is thought to underlie their biochemical "redundancy." Their receptors are part of a larger seven-transmembrane receptor superfamily, commonly referred to as G protein-coupled receptors, which have been demonstrated to be able to signal ...
Sudarshan Rajagopal, James J Campbell
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