Results 1 to 10 of about 185,950 (192)
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 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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Biased Signaling of Protease-activated Receptors [PDF]
Frontiers in Endocrinology, 2014 In addition to their role in protein degradation and digestion, proteases can also function as hormone-like signaling molecules that regulate vital patho-physiological processes, including inflammation, hemostasis, pain and repair mechanisms.
Peishen eZhao +3 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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Corrigendum: Biased signaling of protease-activated receptors [PDF]
Frontiers in Endocrinology, 2015 Figure Figure33 shows a snake diagram of the N-terminal amino acid sequence of human protease-activated receptor (PAR2). It indicates the sites at which different proteases cleave PAR2. These sites are correct. The error is that we accidentally repeated a sequence of amino acid residues (11–16, GAAILL) in positions 17–22 of the snake diagram.
Peishen eZhao +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 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 by endogenous opioid peptides. [PDF]
Proc Natl Acad Sci U S A, 2020 Significance There are >20 different endogenous opioid peptides derived from the three precursors proopiomelanocortin, proenkephalin, and prodynorphin; a long-standing question is the biological utility of having this variety of peptides.
Gomes I +7 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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Biased Signaling in Psychedelic Action. [PDF]
Annu Rev Pharmacol ToxicolPsychedelics show tremendous promise for treating psychiatric disorders and other illnesses, including pain and migraine. Despite decades of research, there is uncertainty which signaling mechanisms are necessary for rapid-acting and durable therapeutic effects of psychedelics.
Wacker D, McCorvy JD.
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