• A2AR
  • In this role, A2AR functions similarly to programmed cell death-1 (PD-1) and cytotoxic t-lymphocyte associated protein-4 (CTLA-4) receptors, namely to suppress immunologic response and prevent associated tissue damage. (wikipedia.org)
  • While several A2A receptor antagonists have progressed to clinical trials for the treatment of Parkinson's disease, A2AR blockade in the context of cancer is less characterized. (wikipedia.org)
  • Mice treated with A2AR antagonists, such as ZM241385 (listed above) or caffeine, show significantly delayed tumor growth due to T-cells resistant to inhibition. (wikipedia.org)
  • This may be now possible because of the recent demonstration that genetic deletion of immunosuppressive A2A and A2B adenosine receptors (A2AR and A2BR) or their pharmacological inactivation can prevent the inhibition of anti-tumor T cells by the hypoxic tumor microenvironment and as a result facilitate full tumor rejection [Ohta A, Gorelik E, Prasad SJ et al (2006) Proc Natl Acad Sci USA 103(35):13132- (pubmedcentralcanada.ca)
  • GPCR
  • This protein is a member of the G protein-coupled receptor (GPCR) family which possess seven transmembrane alpha helices. (wikipedia.org)
  • 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)
  • Receptor homodimers - which consist of two identical GPCRs - are the simplest homomeric GPCR oligomers. (wikipedia.org)
  • Receptor heterodimers - which consist of two different GPCRs - are the simplest heteromeric GPCR oligomers. (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)
  • Perfusion
  • However, in altered cardiac function, such as hypoperfusion caused by hypotension, heart attack or cardiac arrest caused by nonperfusing bradycardias, adenosine has a negative effect on physiological functioning by preventing necessary compensatory increases in heart rate and blood pressure that attempt to maintain cerebral perfusion. (wikipedia.org)
  • Adenosine is used as an adjunct to thallous (thallium) chloride TI 201 or Tc99m myocardial perfusion scintigraphy (nuclear stress test) in patients unable to undergo adequate stress testing with exercise. (wikipedia.org)
  • nucleoside
  • The non-adenosine nucleoside guanosine (Guo) was demonstrated to decrease quinolinic acid(QA)-induced seizures, spontaneously emerged absence epileptic seizures and lipopolysaccharide(LPS)-evoked induction of absence epileptic seizures suggesting its antiepileptic potential. (nih.gov)
  • In the central nervous system, the nucleoside adenosine regulates neuronal activity by modulating the actions of other neurotransmitter systems, thereby influencing many different physiological processes and behaviors. (ke-i.org)
  • A recent study using mice lacking the equilibrative nucleoside transporter 1, a well-established animal model of alcohol addiction, suggests an expanded role for adenosine in cellular and behavioral circadian timing and alcohol intake, particularly during chronodisruption. (ke-i.org)
  • Adenosine is a purine nucleoside composed of a molecule of adenine attached to a ribose sugar molecule (ribofuranose) moiety via a β-N9-glycosidic bond. (wikipedia.org)
  • inhibition
  • Receptor knockouts or pharmacological inhibition in the adenosine, PG/lipoxygenase, lysophosphatidylcholine, and sphingosine-1-phosphate pathways did not individually alter naive T cell migration. (ox.ac.uk)
  • The bronchodilatory action of dyphylline, as with other xanthines, is thought to be mediated through competitive inhibition of phosphodiesterase with a resulting increase in cyclic AMP producing relaxation of bronchial smooth muscle as well as antagonism of adenosine receptors. (drugbank.ca)
  • DP1 gene knockout and/or DP1 inhibition by receptor antagonists markedly reduces airway inflammation, obstruction, hypersensitivity, and pro-allergic cytokine and chemokine production in a mouse model of ovalbumin-induced asthma as well as allergic symptoms in a guinea pig model of allergic conjunctivitis, rhinitis, and asthma. (wikipedia.org)
  • basal
  • The encoded protein (the A2A receptor) is abundant in basal ganglia, vasculature, T lymphocytes, and platelets and it is a major target of caffeine, which is a competitive antagonist of this protein. (wikipedia.org)
  • caffeine
  • Caffeine may reduce cerebral blood flow in premature infants, it is presumed by blocking vascular A2 ARs. (wikipedia.org)
  • Adenosine and caffeine modulate circadian rhythms in the Syrian hamster. (ke-i.org)
  • myocardial
  • As with the A1, the A2A receptors are believed to play a role in regulating myocardial oxygen consumption and coronary blood flow. (wikipedia.org)
  • The A2A receptor is responsible for regulating myocardial blood flow by vasodilating the coronary arteries, which increases blood flow to the myocardium, but may lead to hypotension. (wikipedia.org)
  • Effects of electroacupuncture on the expression of adenosine receptors in the heart tissue of myocardial ischemia rats]. (readbyqxmd.com)
  • To explore the impact of electroacupuncture (EA) on the protein expression of adenosine receptors in the heart of the rats with myocardial ischemia (MI). (readbyqxmd.com)
  • More specifically, A1 and A2A receptors play a role in regulating myocardial oxygen consumption and coronary blood flow . (axonmedchem.com)
  • Recently, clinical evidence was found for the A3 receptor to be involved in rheumatoid arthritis , among other myocardial functions. (axonmedchem.com)
  • cannabinoid
  • However, it has become clear that not all effects of cannabinoid drugs are attributable to their interaction with CB1 and CB2 receptors. (frontiersin.org)
  • Considering the CNS and cancer together allow identification of non-cannabinoid receptor targets that are shared and divergent in both systems. (frontiersin.org)
  • The actions of cannabinoids are also regulated by the endocannabinoid system (ECS) which includes enzymes involved in synthesis, uptake and degradation of endogenous cannabinoid ligands, and the CB1 and CB2 receptors. (frontiersin.org)
  • whereas
  • The contractions to ATP and αβ-meATP were attributed to actions at P2X1 receptors on the vascular smooth muscle, whereas it was shown for the first time that UTP induced an endothelium-dependent vasoconstriction which may involve P2Y2 and/or P2Y4 receptors. (nottingham.ac.uk)
  • pathways
  • Here, we investigated the role of the A2B adenosine receptor (A2BAR) and its associated signaling pathways in governing the proliferation and viability of breast cancer cell line derived CSCs. (readbyqxmd.com)
  • potent
  • L-644,698, BW 245C, BW A868C, and ZK 110841, have been synthesized, found to be about as potent as PGD2 in binding to and stimulating DP1, and used to study the function of this receptor. (wikipedia.org)
  • functional
  • For a long time it was assumed that receptors transmitted their effects exclusively from their basic functional forms - as monomers. (wikipedia.org)
  • In 2005, further evidence was provided that receptor oligomizeration plays a functional role in a living organism with regulatory implication. (wikipedia.org)
  • The functional character of a receptor is dependent on its tertiary or quaternary structure. (wikipedia.org)
  • coronary
  • This feature allows physicians to use adenosine to test for blockages in the coronary arteries, by exaggerating the difference between the normal and abnormal segments. (wikipedia.org)
  • The administration of adenosine also reduces blood flow to coronary arteries past the occlusion. (wikipedia.org)
  • Other coronary arteries dilate when adenosine is administered while the segment past the occlusion is already maximally dilated. (wikipedia.org)
  • actions
  • Endothelium removal and DUP 697, a cyclooxygenase-2 inhibitor, had no significant effect on contraction to ATP but attenuated that to UTP, indicating actions at distinct receptors. (nottingham.ac.uk)
  • interact
  • At the beginning of the 1980s, it was hypothesized, receptors could form larger complexes, the so-called mosaic form, where two receptors may interact directly with each other. (wikipedia.org)
  • Can different receptors interact directly with each other? (wikipedia.org)
  • synthetic and other types of cannabinoids (many developed seeking modulators of other signaling systems, but found to interact with the classic CB1 and/or CB2 receptors). (frontiersin.org)
  • 1993
  • Maggio and co-workers showed in 1993 the ability of the muscarinic M3 receptor and α2C-adrenoceptor to heterodimerize. (wikipedia.org)
  • evidence
  • 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)
  • Clinical evidence for utilization of the A3 adenosine receptor as a target to treat rheumatoid arthritis: data from a phase II clinical trial. (axonmedchem.com)
  • cardiac
  • Just as in A1 receptors, this normally serves as a protective mechanism, but may be destructive in altered cardiac function. (wikipedia.org)
  • This effect on the A1 receptor also explains why there is a brief moment of cardiac standstill when adenosine is administered as a rapid IV push during cardiac resuscitation. (wikipedia.org)
  • activity
  • Adenosine gates glutamatergic input to the circadian clock located in the suprachiasmatic nucleus of the hypothalamus, modulating both photic (light-induced) and nonphotic (behaviorally-induced) synchronization of circadian activity rhythms. (ke-i.org)