Adenosine A2A receptor

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Contents

Function

Adenosine A2A receptor (A2AR) is one of the G protein-coupled receptors. The protein uses adenosine as the preferred endogenous agonist and is involved in increasing intracellular cAMP levels.[1]

Disease

A2AR antagonists are being tested in the treatment of Alzheimer's Disease.

Relevance

A2AR is responsible for regulating myocardial blood flow. It is involved in cerebral and renal blood flow, immune function, pain regulation and sleep. For details see G protein-coupled receptor. A2AR is blocked by caffeine producing the arousal effect.[2] For details see Caffeine.

See also:

Structural highlights

Like other G proteins, A2AR has 7 transmembrane helices.

  • A2AR has a ligand-binding cavity.
  • Adenosine binding site.

3D Structures of adenosine A2A receptor

Adenosine A2A receptor 3D structures


Human A2AR (mutant) complex with adenosine 2ydo

Drag the structure with the mouse to rotate


References

  1. Lebon G, Warne T, Edwards PC, Bennett K, Langmead CJ, Leslie AG, Tate CG. Agonist-bound adenosine A(2A) receptor structures reveal common features of GPCR activation. Nature. 2011 May 18. PMID:21593763 doi:10.1038/nature10136
  2. Lazarus M, Shen HY, Cherasse Y, Qu WM, Huang ZL, Bass CE, Winsky-Sommerer R, Semba K, Fredholm BB, Boison D, Hayaishi O, Urade Y, Chen JF. Arousal effect of caffeine depends on adenosine A2A receptors in the shell of the nucleus accumbens. J Neurosci. 2011 Jul 6;31(27):10067-75. doi: 10.1523/JNEUROSCI.6730-10.2011. PMID:21734299 doi:http://dx.doi.org/10.1523/JNEUROSCI.6730-10.2011

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