- Adenosine A3 receptor
The adenosine A3 receptor, also known as ADORA3, is an
adenosine receptor , but also denotes the humangene encoding it.PBB_Summary
section_title =
summary_text =Function
Adenosine A3 receptors are G-protein-coupled receptors that are involved in a variety of intracellular signaling pathways and physiological functions. It mediates a sustained cardioprotective function during
cardiac ischemia , it is involved in the inhibition ofneutrophil degranulation in neutrophil-mediated tissue injury, it has been implicated in both neuroprotective and neurodegenerative effects, and it may also mediate both cell proliferation and cell death.Gene
Multiple transcript variants encoding different isoforms have been found for this gene.cite web | title = Entrez Gene: ADORA3 adenosine A3 receptor| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=140| accessdate = ]
Therapeutic implications
An adenosine A3 receptor agonist (CF-101) is in clinical trials for the treatment of
rheumatoid arthritis .cite journal
author=Silverman MH, Strand V, Markovits D, "et al"
title=Clinical Evidence for Utilization of the A3 Adenosine Receptor as a Target to Treat Rheumatoid Arthritis: Data from a Phase II Clinical Trial
journal=J Rheumatol
volume=
issue=
pages=
year=2007
pmid=18050382
doi=
url=http://www.jrheum.com/subscribers/07/13/1118.html] In a mouse model of infarction the A3 selective agonist CP-532,903 protected against myocardialischemia andreperfusion injury. cite journal
author=Wan TC, Ge ZD, Tampo A, "et al"
title=The A3 adenosine receptor agonist CP-532,903 protects against myocardial ischemia/reperfusion injury via the sarcolemmal ATP sensitive potassium channel
journal=J Pharmacol Exp Ther
volume=
issue=
pages=
year=2007
pmid=17906066
doi=10.1124/jpet.107.127480
url=http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=17906066]References
Further reading
PBB_Further_reading
citations =
*cite journal | author=Klotz KN |title=Adenosine receptors and their ligands. |journal=Naunyn Schmiedebergs Arch. Pharmacol. |volume=362 |issue= 4-5 |pages= 382–91 |year= 2001 |pmid= 11111832 |doi=
*cite journal | author=Monitto CL, Levitt RC, DiSilvestre D, Holroyd KJ |title=Localization of the A3 adenosine receptor gene (ADORA3) to human chromosome 1p. |journal=Genomics |volume=26 |issue= 3 |pages= 637–8 |year= 1995 |pmid= 7607699 |doi=
*cite journal | author=Salvatore CA, Jacobson MA, Taylor HE, "et al." |title=Molecular cloning and characterization of the human A3 adenosine receptor. |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=90 |issue= 21 |pages= 10365–9 |year= 1993 |pmid= 8234299 |doi=
*cite journal | author=Sajjadi FG, Firestein GS |title=cDNA cloning and sequence analysis of the human A3 adenosine receptor. |journal=Biochim. Biophys. Acta |volume=1179 |issue= 1 |pages= 105–7 |year= 1993 |pmid= 8399349 |doi=
*cite journal | author=Murrison EM, Goodson SJ, Edbrooke MR, Harris CA |title=Cloning and characterisation of the human adenosine A3 receptor gene. |journal=FEBS Lett. |volume=384 |issue= 3 |pages= 243–6 |year= 1996 |pmid= 8617363 |doi=
*cite journal | author=Bonaldo MF, Lennon G, Soares MB |title=Normalization and subtraction: two approaches to facilitate gene discovery. |journal=Genome Res. |volume=6 |issue= 9 |pages= 791–806 |year= 1997 |pmid= 8889548 |doi=
*cite journal | author=Bouma MG, Jeunhomme TM, Boyle DL, "et al." |title=Adenosine inhibits neutrophil degranulation in activated human whole blood: involvement of adenosine A2 and A3 receptors. |journal=J. Immunol. |volume=158 |issue= 11 |pages= 5400–8 |year= 1997 |pmid= 9164961 |doi=
*cite journal | author=Atkinson MR, Townsend-Nicholson A, Nicholl JK, "et al." |title=Cloning, characterisation and chromosomal assignment of the human adenosine A3 receptor (ADORA3) gene. |journal=Neurosci. Res. |volume=29 |issue= 1 |pages= 73–9 |year= 1998 |pmid= 9293494 |doi=
*cite journal | author=Palmer TM, Harris CA, Coote J, Stiles GL |title=Induction of multiple effects on adenylyl cyclase regulation by chronic activation of the human A3 adenosine receptor. |journal=Mol. Pharmacol. |volume=52 |issue= 4 |pages= 632–40 |year= 1997 |pmid= 9380026 |doi=
*cite journal | author=Liang BT, Jacobson KA |title=A physiological role of the adenosine A3 receptor: sustained cardioprotection. |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=95 |issue= 12 |pages= 6995–9 |year= 1998 |pmid= 9618527 |doi=
*cite journal | author=Dougherty C, Barucha J, Schofield PR, "et al." |title=Cardiac myocytes rendered ischemia resistant by expressing the human adenosine A1 or A3 receptor. |journal=FASEB J. |volume=12 |issue= 15 |pages= 1785–92 |year= 1999 |pmid= 9837869 |doi=
*cite journal | author=Murphy WJ, Eizirik E, Johnson WE, "et al." |title=Molecular phylogenetics and the origins of placental mammals. |journal=Nature |volume=409 |issue= 6820 |pages= 614–8 |year= 2001 |pmid= 11214319 |doi= 10.1038/35054550
*cite journal | author=Gao ZG, Chen A, Barak D, "et al." |title=Identification by site-directed mutagenesis of residues involved in ligand recognition and activation of the human A3 adenosine receptor. |journal=J. Biol. Chem. |volume=277 |issue= 21 |pages= 19056–63 |year= 2002 |pmid= 11891221 |doi= 10.1074/jbc.M110960200
*cite journal | author=Broussas M, Cornillet-Lefèbvre P, Potron G, Nguyên P |title=Adenosine inhibits tissue factor expression by LPS-stimulated human monocytes: involvement of the A3 adenosine receptor. |journal=Thromb. Haemost. |volume=88 |issue= 1 |pages= 123–30 |year= 2003 |pmid= 12152652 |doi=
*cite journal | author=Merighi S, Mirandola P, Milani D, "et al." |title=Adenosine receptors as mediators of both cell proliferation and cell death of cultured human melanoma cells. |journal=J. Invest. Dermatol. |volume=119 |issue= 4 |pages= 923–33 |year= 2002 |pmid= 12406340 |doi= 10.1046/j.1523-1747.2002.00111.x
*cite journal | author=Trincavelli ML, Tuscano D, Marroni M, "et al." |title=A3 adenosine receptors in human astrocytoma cells: agonist-mediated desensitization, internalization, and down-regulation. |journal=Mol. Pharmacol. |volume=62 |issue= 6 |pages= 1373–84 |year= 2002 |pmid= 12435805 |doi=
*cite journal | author=Strausberg RL, Feingold EA, Grouse LH, "et al." |title=Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences. |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=99 |issue= 26 |pages= 16899–903 |year= 2003 |pmid= 12477932 |doi= 10.1073/pnas.242603899
*cite journal | author=Feoktistov I, Ryzhov S, Goldstein AE, Biaggioni I |title=Mast cell-mediated stimulation of angiogenesis: cooperative interaction between A2B and A3 adenosine receptors. |journal=Circ. Res. |volume=92 |issue= 5 |pages= 485–92 |year= 2003 |pmid= 12600879 |doi= 10.1161/01.RES.0000061572.10929.2D
*cite journal | author=Gao ZG, Kim SK, Gross AS, "et al." |title=Identification of essential residues involved in the allosteric modulation of the human A(3) adenosine receptor. |journal=Mol. Pharmacol. |volume=63 |issue= 5 |pages= 1021–31 |year= 2003 |pmid= 12695530 |doi=PBB_Controls
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