CB1 Cannabinoid Receptor Signaling and Biased Signaling [PDF]
Molecules, 2021 The CB1 cannabinoid receptor is a G-protein coupled receptor highly expressed throughout the central nervous system that is a promising target for the treatment of various disorders, including anxiety, pain, and neurodegeneration.
Luciana M. Leo, Mary E. Abood
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Biased signaling via serotonin 5-HT2A receptor: From structural aspects to in vitro and in vivo pharmacology [PDF]
Acta Pharmaceutica Sinica BG protein-coupled receptors (GPCRs) represent key drug targets, with approximately 30%–40% of all medications acting on these receptors. Recent advancements have uncovered the complexity of GPCR signaling, including biased signaling, which allows ...
Michał K. Jastrzębski +11 more
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Biased Signaling and Allosteric Modulation at the FSHR [PDF]
Frontiers in Endocrinology, 2019 Knowledge on G protein-coupled receptor (GPCRs) structure and mechanism of activation has profoundly evolved over the past years. The way drugs targeting this family of receptors are discovered and used has also changed.
Flavie Landomiel +10 more
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From theory to platelets: unraveling the history and complexities of biased signaling [PDF]
Blood Vessels, Thrombosis & Hemostasis: Biased signaling refers to a phenomenon where a ligand preferentially activates 1 signaling pathway over another at the same receptor. It is best described for ligands that selectively activate G protein–coupled receptors through G protein or β ...
NaShea C. Kendrick +3 more
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Loss of biased signaling at a G protein-coupled receptor in overexpressed systems. [PDF]
PLoS ONE, 2023 G protein-coupled receptors (GPCRs) regulate cellular signaling pathways by coupling to two classes of transducers: heterotrimeric G proteins and β-arrestins.
Angus Li +4 more
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Biased and G protein-independent signaling of chemokine receptors
Frontiers in Immunology, 2014 Biased signaling or functional selectivity occurs when a 7TM receptor preferentially activates one of several available pathways. It can be divided into three distinct forms: ligand bias, receptor bias, and tissue or cell bias, where it is mediated by ...
Anne eSteen +3 more
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A GLP-1 analogue optimized for cAMP-biased signaling improves weight loss in obese mice [PDF]
Molecular MetabolismObjective: Glucagon-like peptide 1 (GLP-1) receptor (GLP-1R) agonism is foundational to modern obesity pharmacotherapies. These compounds were engineered for maximal G protein alpha(s) (Gsα) signaling potency and downstream cAMP production. However, this
Jonathan D. Douros +21 more
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Molecular mechanisms of fentanyl mediated β-arrestin biased signaling. [PDF]
PLoS Computational Biology, 2020 The development of novel analgesics with improved safety profiles to combat the opioid epidemic represents a central question to G protein coupled receptor structural biology and pharmacology: What chemical features dictate G protein or β-arrestin ...
Parker W de Waal +7 more
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PD 102807 Induces M3 mAChR-Dependent GRK-/Arrestin-Biased Signaling in Airway Smooth Muscle Cells [PDF]
American Journal of Respiratory Cell and Molecular Biology, 2022 Sushrut D Shah +2 more
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Ubiquitination of GRK2 Is Required for the β-Arrestin-Biased Signaling Pathway of Dopamine D2 Receptors to Activate ERK Kinases [PDF]
International Journal of Molecular Sciences, 2023 Srijan Acharya, Xiaohan Zhang
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