Assessment of biased agonism at the A<sub>3</sub> adenosine receptor using β-arrestin and miniGα<sub>i</sub> recruitment assays. [PDF]
Biochem Pharmacol, 2020 Pottie E +4 more
europepmc +1 more source
Use of Backbone Modification To Enlarge the Spatiotemporal Diversity of Parathyroid Hormone Receptor-1 Signaling via Biased Agonism. [PDF]
J Am Chem Soc, 2019 Liu S +7 more
europepmc +1 more source
New paradigms in adenosine receptor pharmacology: allostery, oligomerization and biased agonism. [PDF]
Br J Pharmacol, 2018 Vecchio EA +5 more
europepmc +1 more source
G protein signaling-biased agonism at the κ-opioid receptor is maintained in striatal neurons. [PDF]
Sci Signal, 2018 Ho JH +5 more
europepmc +1 more source
Biased agonism and opioid receptor-mediated analgesia
Proceedings for Annual Meeting of The Japanese Pharmacological Society, 2018 openaire +2 more sources
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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
exaly +3 more sources
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 ...
Jo-Anne Baltos +2 more
exaly +3 more sources
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
exaly +3 more sources
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.
Hans Brauner-Osborne
exaly +4 more sources
What is pharmacological ‘affinity’? Relevance to biased agonism and antagonism
Trends in Pharmacological Sciences, 2014The differences between affinity measurements made in binding studies and those relevant to receptor function are described. There are theoretical and practical reasons for not utilizing binding data and, in terms of the quantification of signaling bias, it is unnecessary to do so.
exaly +3 more sources