In 2005, further evidence was provided that receptor oligomerization plays a functional role in a living organism with regulatory implication. (wikipedia.org)
The protein expression of nucleotide-binding oligomerization domain-like receptor family pyrin domain-containing 3 (NLRP3), apoptosis speck-like protein (ASC), caspase-1, gasdermin D (GSDMD), and GSDMD-N, the mRNA expression of NLRP3, caspase-1, GSDMD, interleukin-1ß (IL-1ß) and IL-18 were evaluated. (bvsalud.org)
Protein2
A GPCR oligomer is a protein complex that consists of a small number (ὀλίγοι oligoi "a few", μέρος méros "part, piece, component") of G protein-coupled receptors (GPCRs). (wikipedia.org)
This has consequences for: the supply of the cell surface with receptors the ligand binding at corresponding binding sites the G-protein coupling the GPCR-mediated signal transduction modifying the desensitization profile the tendency for endocytosis and internalization the post-endocytotic fate of the receptors There are various methods to detect and observe GPCR oligomers. (wikipedia.org)
Analysis1
The first direct evidence that GPCRs functioned as oligomers in vivo came from Overton and Blumer in 2000 by fluorescence resonance energy transfer (FRET) analysis of the α-factor receptor in the yeast Saccharomyces cerevisiae. (wikipedia.org)
Purine nucleoside3
The endogenous levels of the purine nucleoside, adenosine, increase significantly following cardiovascular events. (frontiersin.org)
The purine nucleoside adenosine was first identified in 1929 when Drury and Szent-Gyorgyi successfully extracted a rhythm-influencing adenylic substance from the mammalian heart and other tissues ( Drury and Szent-Gyorgyi, 1929 ). (frontiersin.org)
Recent studies have built upon decades of evidence that adenosine, a purine nucleoside that can act as a neuromodulator, is involved in pain transmission and sensitization. (mdpi.com)
Agonist2
Studies with CGS21680, a specific agonist of adenosine A2A receptor (AdoRA2A), and ZM241385, an AdoRA2-selective antagonist, indicate that the inhibitory effects of adenosine are mediated via cyclic AMP (cAMP)-elevating AdoRA2A, leading to protein kinase A (PKA) activation. (nih.gov)
Pretreating the isolated pulmonary arteries with DOPA 1 µM enhanced vasoconstriction in response to phenylephrine, an ADRA1 agonist, but not to U-46619, a thromboxane A2 agonist or endothelin-1. (bvsalud.org)
Inhibitors2
Inhibitors of the PKA catalytic subunits (H89 and PKA inhibitor peptide 14-22) failed to abrogate the inhibitory effects of CADO. (nih.gov)
Numerous clinical trials are currently evaluating combination immunomodulatory strategies incorporating vaccine-based therapies, checkpoint inhibitors, and chimeric antigen receptor (CAR) T cells. (encyclopedia.pub)
Protein-coupled2
A GPCR oligomer is a protein complex that consists of a small number (ὀλίγοι oligoi "a few", μέρος méros "part, piece, component") of G protein-coupled receptors (GPCRs). (wikipedia.org)
We previously showed that 3,4-l-dihydroxylphenyalanine (DOPA) sensitizes vasomotor response to sympathetic tone via coupling between the adrenergic receptor alpha1 (ADRA1) and a G protein-coupled receptor 143 (GPR143), a DOPA receptor. (bvsalud.org)
Neurons2
Toll-like receptor 4 signaling in trigeminal ganglion neurons contributes tongue-referred pain associated with tooth pulp inflammation. (medscape.com)
Metabotropic glutamate receptor 1 (mGluR1): antibody specificity and receptor expression in cultured primary neurons. (neurotree.org)
Effector1
mRNA expressions of Notch receptors (Notch1,3) and ligands (Jag1, Dll4), and downstream effector genes (Hey1, MLCK, MYPT1) were assessed by RT-qPCR. (bvsalud.org)
Quaternary1
The functional character of a receptor is dependent on its tertiary or quaternary structure. (wikipedia.org)
Mice1
Toll-like receptor signaling adapter proteins govern spread of neuropathic pain and recovery following nerve injury in male mice. (medscape.com)
Clinical1
Clinical evidence and rodent studies have suggested that adenosine signaling also plays a critical role in migraine headache. (mdpi.com)
Effects6
For a long time it was assumed that receptors transmitted their effects exclusively from their basic functional forms - as monomers. (wikipedia.org)
The goal of this study was to investigate the effects of adenosine and its stable analogue 2-chloroadenosine (CADO) on the cytotoxic activity and cytokine production by human antimelanoma specific CD8+ and CD4+ T-helper type 1 (Th1) clones. (nih.gov)
Using cAMP analogues with different affinities for the A and B sites of the regulatory subunits of PKAI and PKAII, we found that activation of PKAI, but not of PKAII, mimicked the inhibitory effects of adenosine on T-cell cytotoxic activity and cytokine production. (nih.gov)
Adenosine exerts cardioprotective, neuromodulatory, and immunosuppressive effects by activating plasma membrane-bound P1 receptors that are widely expressed in the cardiovascular system. (frontiersin.org)
Here, we provide a comprehensive and up-to-date critical review about the main therapeutic advantages of tuning adenosine signalling pathways in HFpEF, without discounting their side effects and how these can be seized. (frontiersin.org)
Only in 1972, Geoff Burnstock (born: May 10, 1929, died: June 2, 2020) coined the term purinergic signalling referring to the extracellular effects of adenosine 5′-triphosphate (ATP). (frontiersin.org)
Expression1
LPS and TNF alpha modulate AMPA/NMDA receptor subunit expression and induce PGE2 and glutamate release in preterm fetal ovine mixed glial cultures. (medscape.com)
Methods1
This has consequences for: the supply of the cell surface with receptors the ligand binding at corresponding binding sites the G-protein coupling the GPCR-mediated signal transduction modifying the desensitization profile the tendency for endocytosis and internalization the post-endocytotic fate of the receptors There are various methods to detect and observe GPCR oligomers. (wikipedia.org)
Plays1
In 2005, further evidence was provided that receptor oligomerization plays a functional role in a living organism with regulatory implication. (wikipedia.org)
Review1
While initially thought to be a receptor heterodimer, a review from 2015 determined that the A2A-DRD2 heteromer is a heterotetramer composed of A2A and DRD2 homodimers (i.e., two adenosine A2A receptors and two dopamine D2 receptors). (wikipedia.org)
Association1
Erythropoietin improves motor and cognitive deficit, axonal pathology, and neuroinflammation in a combined model of diffuse traumatic brain injury and hypoxia, in association with upregulation of the erythropoietin receptor. (medscape.com)
Role1
Following Burnstock's pioneering work on the role of ATP-sensitive P2 purinoceptors, its metabolite adenosine soon became recognized as an extracellular signalling molecule through the activation of plasma membrane-bound P1 receptors family that are expressed in every organ systems in the body. (frontiersin.org)
Activity1
The cytotoxic activity of CD8+ T cells was inhibited by adenosine and CADO. (nih.gov)
Evidence1
The first direct evidence that GPCRs functioned as oligomers in vivo came from Overton and Blumer in 2000 by fluorescence resonance energy transfer (FRET) analysis of the α-factor receptor in the yeast Saccharomyces cerevisiae. (wikipedia.org)
Type1
A novel autoantibody against ephrin type B receptor 2 in acute necrotizing encephalopathy. (medscape.com)
Drugs1
The existence of receptor oligomers is a general phenomenon, whose discovery has superseded the prevailing paradigmatic concept of the function of receptors as plain monomers, and has far-reaching implications for the understanding of neurobiological diseases as well as for the development of drugs. (wikipedia.org)