Results 201 to 210 of about 11,641 (225)
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2022
This chapter considers biased signaling as a natural function of G protein-coupled receptors (GPCRs) in the form of probe dependence. Thus, any ligand that changes the conformation of the receptor (agonist, antagonist, or allosteric modulator) has the potential to change the natural signaling of the receptor through unequal conformational alterations ...
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This chapter considers biased signaling as a natural function of G protein-coupled receptors (GPCRs) in the form of probe dependence. Thus, any ligand that changes the conformation of the receptor (agonist, antagonist, or allosteric modulator) has the potential to change the natural signaling of the receptor through unequal conformational alterations ...
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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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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 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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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
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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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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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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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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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