Results 161 to 170 of about 11,411 (182)
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Novel pathways in gonadotropin receptor signaling and biased agonism
Reviews in Endocrine and Metabolic Disorders, 2011Gonadotropins play a central role in the control of male and female reproduction. Selective agonists and antagonists of gonadotropin receptors would be of great interest for the treatment of infertility or as non steroidal contraceptive. However, to date, only native hormones are being used in assisted reproduction technologies as there is no ...
Ulloa-Aguirre, Alfredo +4 more
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Emergent biological properties of arrestin pathway-selective biased agonism
Journal of Receptors and Signal Transduction, 2013Our growing appreciation of the pluridimensionality of G protein-coupled receptor (GPCR) signaling, combined with the phenomenon of orthosteric ligand "bias", has created the possibility of drugs that selectively modulate different aspects of GPCR function for therapeutic benefit. When viewed from the short-term perspective, e.g.
Kathryn M, Appleton, Louis M, Luttrell
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Biased Agonism of the Angiotensin II Type 1 Receptor
Mini-Reviews in Medicinal Chemistry, 2012G protein-coupled receptors (GPCRs) can be activated by multiple ligands and exhibit the capacity to couple to numerous intracellular signal transduction pathways. This property allows GPCRs to be modulated by biased agonists that selectively activate specific subsets of GPCR-regulated cellular signaling proteins.
C M, Godin, S S G, Ferguson
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A kinetic view of GPCR allostery and biased agonism
Nature Chemical Biology, 2017G-protein-coupled receptors (GPCRs) are one of the most tractable classes of drug targets. These dynamic proteins can adopt multiple active states that are linked to distinct functional outcomes. Such states can be differentially stabilized by ligands interacting with the endogenous agonist-binding orthosteric site and/or by ligands acting via ...
J Robert Lane +4 more
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Biased agonism at the µ-opioid receptor
2017The μ opioid receptor (MOP) is the main therapeutic target for the most clinically useful class of analgesics for treating severe acute and chronic pain, despite the numerous associated side effects that limit their use. The property of G protein-coupled receptors (GPCRs) where different ligands stabilise the receptor into unique active conformations ...
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Biased Agonism in Incretin-based Therapies
International Journal of Clinical Metabolism and DiabetesAround one-third of clinical drugs used today target G protein-coupled receptors (GPCRs). The action of hormones at GPCRs leads to downstream events predominantly mediated by cAMP through the activation of G proteins. The beta-arrestin (BA) pathway serves to recycle the receptor and desensitize the cell surface.
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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.
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Understanding biased agonism at the dopamine D₂ receptor
2017The phenomenon of “biased agonism” presents an attractive avenue for drug development as it allows the separation of therapeutic effects from side effects mediated by the same target. A prototypical G protein-coupled receptor at which biased agonism has been extensively studied is the dopamine D₂ receptor, an important therapeutic target for current ...
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