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Adenosine A3 receptor

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Adenosine A3 receptor

Adenosine A3 receptor
Available structures
PDB Ortholog search: RCSB
Identifiers
ADORA3 Gene
RNA expression pattern

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

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. Recent publications demonstrate that adenosine A3 receptor antagonists (SSR161421) could have therapeutic potencial in bronchial asthma (17,18).

Gene

Multiple transcript variants encoding different isoforms have been found for this gene.[1]

Therapeutic implications

An adenosine A3 receptor agonist (CF-101) is in clinical trials for the treatment of rheumatoid arthritis.[2] In a mouse model of infarction the A3 selective agonist CP-532,903 protected against myocardial ischemia and reperfusion injury.[3]

Selective Ligands

A number of selective A3 ligands are available.[4][5][6][7][8][9][10][11][12][13][14][15]

Agonists/Positive Allosteric Modulators

  • 2-(1-Hexynyl)-N-methyladenosine
  • CF-101 (IB-MECA)
  • CF-102
  • 2-Cl-IB-MECA
  • CP-532,903
  • Inosine[16]
  • LUF-6000
  • MRS-3558

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[17][18]

Inverse Agonists

References

Further reading

External links

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