Structural basis for the constitutive activity and immunomodulatory properties of the Epstein-Barr virus-encoded G protein-coupled receptor BILF1.
Sign Up to like & getrecommendations! Published in 2021 at "Immunity"
DOI: 10.1016/j.immuni.2021.06.001
Abstract: Epstein-Barr virus (EBV) encodes a G protein-coupled receptor (GPCR) termed BILF1 that is essential for EBV-mediated immunosuppression and oncogenesis. BILF1 couples with inhibitory G protein (Gi), the major intracellular signaling effector for human chemokine receptors,… read more here.
Keywords: epstein barr; constitutive activity; barr virus; bilf1 ... See more keywords
Constitutive activity of 5-HT receptors: Factual analysis
Sign Up to like & getrecommendations! Published in 2020 at "Neuropharmacology"
DOI: 10.1016/j.neuropharm.2020.107967
Abstract: The constitutive activity of different serotonin receptors (5-HTRs) toward intracellular signaling pathways has been proposed to have physiological and pathological importance. Inverse agonists block the constitutive activity and can be used to probe and silence… read more here.
Keywords: constitutive activity; receptors factual; activity htrs; activity ... See more keywords
Structural insights into constitutive activity of 5-HT6 receptor.
Sign Up to like & getrecommendations! Published in 2023 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.2209917120
Abstract: While most therapeutic research on G-protein-coupled receptors (GPCRs) focuses on receptor activation by (endogenous) agonists, significant therapeutic potential exists through agonist-independent intrinsic constitutive activity that can occur in various physiological and pathophysiological settings. For example,… read more here.
Keywords: insights constitutive; structural insights; constitutive activity; ht6r ... See more keywords
Is the 5-hydroxytryptamine 7 Receptor Constitutively Active in the Vasculature? A Study in Veins/Vein
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Cardiovascular Pharmacology"
DOI: 10.1097/fjc.0000000000001296
Abstract: Abstract: The 5-hydroxytryptamine 7 (5-HT7) receptor is reported to have considerable constitutive activity when transfected into cells. Constitutive activity—receptor activity in the absence of known agonist—is important for understanding the contributions of a receptor to… read more here.
Keywords: ht7 receptor; constitutive activity; contraction; vena cava ... See more keywords
Constitutive activity of the dopamine (D5) receptor, highly expressed in CA1 hippocampal neurons, selectively reduces CaV3.2 and CaV3.3 currents
Sign Up to like & getrecommendations! Published in 2022 at "British Journal of Pharmacology"
DOI: 10.1111/bph.16006
Abstract: CaV3.1‐3 currents differentially contribute to neuronal firing patterns. CaV3 are regulated by G protein‐coupled receptors (GPCRs) activity, but information about CaV3 as targets of the constitutive activity of GPCRs is scarce. We investigate the impact… read more here.
Keywords: activity dopamine; dopamine receptor; constitutive activity; cav3 currents ... See more keywords
The GPCR accessory protein MRAP2 regulates both biased signaling and constitutive activity of the ghrelin receptor GHSR1a
Sign Up to like & getrecommendations! Published in 2020 at "Science Signaling"
DOI: 10.1126/scisignal.aax4569
Abstract: An accessory protein suppresses β-arrestin–dependent signaling and constitutive activity of the ghrelin receptor. Skewing signaling with an accessory protein Ghrelin is a peptide that is secreted by the stomach during fasting to promote food intake.… read more here.
Keywords: protein; accessory protein; constitutive activity; ghsr1a ... See more keywords
Pharmacoperone rescue of vasopressin 2 receptor mutants reveals unexpected constitutive activity and coupling bias
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DOI: 10.1371/journal.pone.0181830
Abstract: Pharmacoperones are small molecules that diffuse into cells and rescue misfolded, mistrafficked protein mutants, restoring their function. These substances act with high target specificity, serving as templates to fold (or refold) receptors, enzymes, ion channels… read more here.
Keywords: receptor mutants; pharmacoperone; constitutive activity; rescue ... See more keywords
The Constitutive Activity of Spinal 5-HT6 Receptors Contributes to Diabetic Neuropathic Pain in Rats
Sign Up to like & getrecommendations! Published in 2023 at "Biomolecules"
DOI: 10.3390/biom13020364
Abstract: Diabetic neuropathy is often associated with chronic pain. Serotonin type 6 (5-HT6) receptor ligands, particularly inverse agonists, have strong analgesic potential and may be new candidates for treating diabetic neuropathic pain and associated co-morbid cognitive… read more here.
Keywords: diabetic neuropathic; constitutive activity; neuropathic pain; pain ... See more keywords