Results 151 to 160 of about 11,411 (182)
A Complementary Scale of Biased Agonism for Agonists with Differing Maximal Responses. [PDF]
Sci Rep, 2017 Burgueño J +6 more
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Conceptual and experimental issues in biased agonism
Cellular Signalling, 2021In this review, we discuss the theoretical and experimental foundations for assessing agonism in the context of signalling bias in GPCRs. We show that the formulation of efficacy in classical receptor theory and the definition of ligand-induced allosteric effect in chemical thermodynamics are coincident measures of agonism, only if we recognize that ...
H Ongun, Onaran, Tommaso, Costa
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Biased agonism of the calcium-sensing receptor
Cell Calcium, 2012After the discovery of molecules modulating G protein-coupled receptors (GPCRs) that are able to selectively affect one signaling pathway over others for a specific GPCR, thereby "biasing" the signaling, it has become obvious that the original model of GPCRs existing in either an "on" or "off" conformation is too simple.
Thomsen, Alex Rojas Bie +2 more
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Biased agonism at adenosine receptors
Cellular Signalling, 2021Adenosine modulates many aspects of human physiology and pathophysiology through binding to the adenosine family of G protein-coupled receptors, which are comprised of four subtypes, the A1R, A2AR, A2BR and A3R. Modulation of adenosine receptor function by exogenous agonists, antagonists and allosteric modulators can be beneficial for a number of ...
Samantha M, McNeill +3 more
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Biased Agonism and Biased Allosteric Modulation at the CB1 Cannabinoid Receptor
Molecular Pharmacology, 2015CB1 cannabinoid receptors (CB1Rs) are attractive therapeutic targets for numerous central nervous system disorders. However, clinical application of cannabinoid ligands has been hampered owing to their adverse on-target effects. Ligand-biased signaling from, and allosteric modulation of, CB1Rs offer pharmacological approaches that may enable the ...
Elham, Khajehali +5 more
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Encoding mu-opioid receptor biased agonism with interaction fingerprints
Journal of Computer-Aided Molecular Design, 2021Opioids are potent painkillers, however, their therapeutic use requires close medical monitoring to diminish the risk of severe adverse effects. The G-protein biased agonists of the μ-opioid receptor (MOR) have shown safer therapeutic profiles than non-biased ligands.
R. Bruno Hernández-Alvarado +5 more
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Biased Agonism: The Future (and Present) of Inotropic Support
Journal of Cardiothoracic and Vascular Anesthesia, 2020Biased agonism, which is the concept that different ligands activate different downstream signalling partners in different ratios to cause different functional effects, is yet to gain appropriate appreciation in the field of inotropic pharmacology. Biased agonism has already proven to be a clinically translatable technology in analgesic pharmacology ...
Huw Garland, Alain Vuylsteke
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Biased agonism in the mu-opioid receptor
2021Dr. Karina Martinez-Mayorga discuss Biased agonism in the mu-opioid receptor.
Karina Martinez-Mayorga +2 more
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Biased Agonism at MOP Opioid Receptors
2023Opioids are the mainstay of pain management. Their use comes with side effects such as respiratory depression, constipation, addiction and tolerance. Opioids interact with opioid receptors; classical μ (MOP), δ (DOP) and κ (KOP) and non-classical N/OFQ receptor or NOP. Classical is naloxone sensitive and the main target for clinical opioid medications.
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2018
Agonists and most natural ligands bind to receptors in their inactive state and quickly induce an active receptor conformation that initiates cell signaling. The active receptor state initiates signaling because of its structural complementariness with coupling proteins that activate signaling pathways, such as G proteins and G protein-coupled receptor
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Agonists and most natural ligands bind to receptors in their inactive state and quickly induce an active receptor conformation that initiates cell signaling. The active receptor state initiates signaling because of its structural complementariness with coupling proteins that activate signaling pathways, such as G proteins and G protein-coupled receptor
openaire +2 more sources