Adenosine A3 receptor

The adenosine A₃ receptor, also known as ADORA3, is an adenosine receptor, but also denotes the human gene encoding it.

ADORA3
Available structures PDB Ortholog search: PDBe RCSB List of PDB id codes 1OEA, 1R7N
Identifiers
Aliases	ADORA3, A3AR, AD026, bA552M11.5, adenosine A3 receptor
External IDs	OMIM: 600445; MGI: 104847; HomoloGene: 550; GeneCards: ADORA3; OMA:ADORA3 - orthologs
Gene location (Human) Chr. Chromosome 1 (human)[1] Band 1p13.2 Start 111,499,429 bp[1] End 111,503,633 bp[1]
Gene location (Mouse) Chr. Chromosome 3 (mouse)[2] Band 3 F2.2|3 46.45 cM Start 105,778,174 bp[2] End 105,816,242 bp[2]
RNA expression pattern Bgee Human Mouse (ortholog) Top expressed in C1 segment right adrenal cortex left adrenal gland left adrenal cortex inferior ganglion of vagus nerve mucosa of transverse colon substantia nigra Descending thoracic aorta gallbladder internal globus pallidus Top expressed in granulocyte spermatid embryo red pulp morula blastocyst lip dermis dentate gyrus of hippocampal formation granule cell superior frontal gyrus More reference expression data BioGPS More reference expression data
Gene ontology Molecular function G protein-coupled adenosine receptor activity G protein-coupled receptor activity signal transducer activity Cellular component integral component of membrane plasma membrane membrane integral component of plasma membrane Biological process G protein-coupled adenosine receptor signaling pathway inflammatory response signal transduction activation of adenylate cyclase activity regulation of heart contraction response to wounding negative regulation of cell population proliferation negative regulation of cell migration negative regulation of NF-kappaB transcription factor activity G protein-coupled receptor signaling pathway Sources:Amigo / QuickGO
Orthologs Species Human Mouse Entrez 140 11542 Ensembl ENSG00000282608 ENSMUSG00000000562 UniProt P0DMS8 Q61618 Q3U4C5 RefSeq (mRNA) NM_001302679 NM_000677 NM_001302678 NM_009631 RefSeq (protein) NP_000668 NP_001289607 NP_001289608 NP_033761 Location (UCSC) Chr 1: 111.5 – 111.5 Mb Chr 3: 105.78 – 105.82 Mb PubMed search [3] [4]
Wikidata
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Function

Adenosine A₃ receptors are G protein-coupled receptors that couple to Gi/Gq and 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 of neutrophil 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^{[citation needed]}. Recent publications demonstrate that adenosine A3 receptor antagonists (SSR161421) could have therapeutic potential in bronchial asthma (17,18).

Gene

Multiple transcript variants encoding different isoforms have been found for this gene.^[5]

Therapeutic implications

An adenosine A₃ receptor agonist (CF-101) is in clinical trials for the treatment of rheumatoid arthritis.^[6] In a mouse model of infarction the A₃ selective agonist CP-532,903 protected against myocardial ischemia and reperfusion injury.^[7]

Selective Ligands

A number of selective A₃ ligands are available.^{[8][9][10][11][12][13][14][15][16][17][18][19][20]}

Agonists/Positive Allosteric Modulators

• 2-(1-Hexynyl)-N-methyladenosine
• CF-101 (IB-MECA)/Piclidenoson
• CF-102 (2-Cl-IB-MECA)/Namodenoson
• CP-532,903
• Inosine^[21]
• LUF-6000^[22]
• MRS-3558
• MRS7292
• AST-004
• CF 602

Antagonists/Negative Allosteric Modulators

• KF-26777
• MRS-545
• MRS-1191
• MRS-1220
• MRS-1334
• MRS-1523
• MRS-3777
• MRE-3005-F20
• MRE-3008-F20
• PSB-11
• OT-7999
• VUF-5574
• SSR161421^[23][24]
• ISAM-DM10

Inverse Agonists

• PSB-10