Adenosine A3 receptor

Cell surface receptor found in humans From Wikipedia, the free encyclopedia

Adenosine A3 receptor

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

Quick Facts ADORA3, Available structures ...
ADORA3
Available structures
PDBOrtholog search: PDBe RCSB
Identifiers
AliasesADORA3, A3AR, AD026, bA552M11.5, adenosine A3 receptor
External IDsOMIM: 600445; MGI: 104847; HomoloGene: 550; GeneCards: ADORA3; OMA:ADORA3 - orthologs
Orthologs
SpeciesHumanMouse
Entrez
Ensembl
UniProt
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 MbChr 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

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

References

Further reading

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