Introduction to 2a Adenosine

Regadenoson is a selective agonist of the A2A adenosine receptor which mediates the vasodilative effect of adenosine.

The A2A adenosine receptor colocalized with ezrin, an A-kinase anchoring protein, in the luminal membrane of duct cells in the mouse and guinea pig pancreas.

ABSTRACT Signaling through A2a adenosine receptor specifically prevent pancreatic &bgr;‐cells (PBCs) loses under diabetogenic conditions.

Observation made in our previous work indicated the importance of the carbonyl group of amide in the indolylpyrimidylpiperazine (IPP) for its human A2A adenosine receptor (hA2AAR) subtype binding selectivity over the other AR subtypes.

The structures of proteinase K (PK) and A2A adenosine receptor (A2AAR) were determined to resolutions of 1.

Limited O2 availability leads to increased levels of adenosine, which regulates the kidney via activation of both A1 and A2A adenosine receptors (A1R and A2AR, respectively).

Here, using long-timescale classical all-atom molecular dynamics simulations, we explore, in atomic detail, the motion of sodium ions within the ligand-binding pocket of the A2A adenosine receptor (A2A-AR) both in the presence and absence of ligands and in the active and inactive state.

These inhibitory effects were mainly mediated by up-regulating cAMP/PKA pathway, where CoQ10 stimulated the A2A adenosine receptor and decreased phosphodiesterase 3A phosphorylation.

Methods and aims: Using a well-characterized animal model of binge eating, we investigated the epigenetic regulation of the A2A Adenosine Receptor (A2AAR) and dopaminergic D2 receptor (D2R) genes.

Recent studies have highlighted the fundamental role of A2a adenosine receptor (A2aR) in potentiation of insulin secretion and proliferation of PBCs.

Long-term studies of anti-pathogen and anti-tumor immunity have provided complementary genetic and pharmacological evidence for the immunosuppressive and immunomodulatory effects of Hypoxia-HIF-1α and adenosine-mediated suppression via the A2A adenosine receptor signaling pathway (Hypoxia-A2A-adenosinergic).

New 8-amino-6-aryl-2-phenyl-1,2,4-triazolo[4,3-a]pyrazine-3-ones were designed to obtain dual antioxidant-human A2A adenosine receptor (hA2A AR) antagonists.

Microcrystals of human A2A adenosine receptor and proteinase K were screened and the structures determined to resolutions of 4.

Using chemical screening and in vivo imaging, we discovered that inhibition of A2a adenosine receptors (ARs) causes ectopic OPC migration out of the spinal cord.

The method has been applied to 17 ligands of the A2A adenosine receptor, all with published experimental kinetic binding data.

To obtain potential A2A adenosine receptor agonists, a series of 2-hydrazinyladenosine derivatives were synthesized and assayed for adenosine receptors activity using radioligand binding activity assays.

Several classes of candidate compounds have emerged, including inhibitors of the adenosine axis, specifically A2A adenosine receptor antagonists.

This high-throughput, label-free and quantitative affinity MS screen resulted in discovery of three new antagonists of the A2A adenosine receptor.

Two 15 μsec all-atom simulations of the A2A adenosine receptor were obtained in a ternary mixture of cholesterol, saturated, and unsaturated phosphatidyl choline lipids.

We also assessed the involvement of A1 and A2A adenosine receptors and phosphatidylinositol-3 kinase (PI3K), MAPK, and protein kinase C (PKC) signaling pathways on the guanosine effects.

Crystal structures for the antagonist-bound [146, 305, 213, 55], agonist-bound [362, 196, 198] and G protein-bound A2A adenosine receptors [43] have been described.

Uric acid, interacting with A1 and A2a adenosine receptors as well as phosphodiesterase and Na,K-ATPase of neurons, modulates the activity of nerve centers, which in turn modulate immunocytes.

AbbreviationsA2A adenosine receptorDPPC dipalmitoyl phosphatidylcholineecd extracellular domainecl2 extracellular loop 2eLRR extracellular Leucine rich repeat domainflaD flagellin of Vibrio choleraefliC flagellin of Salmonella typhimuriumHPV hyper-variableMD molecular dynamicsRMSD root means squared deviationTIR toll-interleukin receptorTLR5 toll like receptor 5VPAC1 vasoactive intestinal peptide receptor Communicated by Ramaswamy H.

CD73 and other nucleotidases/phosphatases dephosphorylate and convert extracellular AMP into adenosine, which binds the A2A adenosine receptor (A2aR).

Considering the estimated IC50 value, UK 432097, showing a relatively high binding affinity to the A2A adenosine receptor, has been identified as the most potent anti-aggregatory agent.

In particular, A2A adenosine receptor (A2AR), one of the G-protein-coupled-receptors, exhibits immunosuppressive functions.

N9-Benzyl-substituted imidazo-, pyrimido- and 1,3-diazepino[2,1-f]purinediones were designed as dual-target-directed ligands combining A2A adenosine receptor (AR) antagonistic activity with blockade of monoamine oxidase B (MAO-B).

Selective A1 and A2A adenosine receptor antagonists, or their combination, did not have any effect.

Blocking A2A adenosine receptors by ZM241385 abolished the effect of BDNF, whereas additional stimulation of A2A receptors by CGS21680 increased MEPP amplitudes, which was prevented by MEK1/2 inhibitor U0126.

In this work, an enlarged series of 1,2,4-triazolo[4,3-a]pyrazin-3-ones was designed to target the human (h) A2A adenosine receptor (AR) or both hA1 and hA2A ARs.

PURPOSE Caffeine is a non-selective antagonist of A1 and A2A adenosine receptors (ARs).

A causal relationship has been described for adenosine-activation of A2A adenosine receptors, hCAT-1, and eNOS activity (i.

In contrast, pretreatment with an A2A adenosine receptor antagonist (SCH 58261 0.

This is illustrated in a number of protein systems extracted from other FEP studies in the literature: inhibitors of CDK2 kinase and a series of A2A adenosine G protein-coupled receptor antagonists, where the results obtained with QligFEP are in excellent agreement with experimental data.

We found an involvement of A2A adenosine receptors, ionotropic glutamate N-methyl-D-aspartate (NMDA), and non-NMDA receptors in the increased number of cerebellar neurons.

We demonstrate the effectiveness of ConDock on well-characterized GPCRs such as the β2 adrenergic and A2A adenosine receptors.

Molecular docking screens against crystal structures of the A2A adenosine and the D4 dopamine receptors were carried out and 53 top-ranked molecules were evaluated experimentally.

Objective To explore the expression of the A2A adenosine receptor and the inflammatory cytokines interleukin-1 beta (IL-1β) and tumor necrosis factor alpha (TNF-α) in human degenerative nucleus pulposus (NP) cells after they have been treated with a pulsed electromagnetic field (PEMF).

By this means, the A2A adenosine receptor was successfully reconstituted into a series of commercial detergents for stabilization screening and nanodiscs for electron microscopy analysis.

In this study, we identified A2a adenosinergic signaling as an important regulator of inflammatory and tumor-associated lymphangiogenesis.