Adenosine A2A receptor

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== Relevance ==
== Relevance ==
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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]].
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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.<ref>PMID:21734299</ref> See [[Caffeine]].
== Structural highlights ==
== Structural highlights ==
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[[2ydv]] – hA2AR (mutant) + agonist<br />
[[2ydv]] – hA2AR (mutant) + agonist<br />
[[3pwh]], [[3rey]], [[3rfm]], [[3uza]], [[3uzc]] – hA2AR (mutant) + antagonist<br />
[[3pwh]], [[3rey]], [[3rfm]], [[3uza]], [[3uzc]] – hA2AR (mutant) + antagonist<br />
 +
[[3rfm]] – hA2AR (mutant) + caffeine<br />
[[3vg9]], [[3vga]] – hA2AR (mutant) + antibody<br />
[[3vg9]], [[3vga]] – hA2AR (mutant) + antibody<br />
[[4eiy]] – hA2AR/cytochrome b562 + antagonist <br />
[[4eiy]] – hA2AR/cytochrome b562 + antagonist <br />

Revision as of 15:39, 5 January 2016

Human A2AR (mutant) complex with adenosine 2ydo

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3D Structures of adenosine A2A receptor

Updated on 05-January-2016

3eml – hA2AR/lysozyme + antagonist – human
3qak – hA2AR/lysozyme + agonist
2ydo – hA2AR (mutant) + adenosine
2ydv – hA2AR (mutant) + agonist
3pwh, 3rey, 3rfm, 3uza, 3uzc – hA2AR (mutant) + antagonist
3rfm – hA2AR (mutant) + caffeine
3vg9, 3vga – hA2AR (mutant) + antibody
4eiy – hA2AR/cytochrome b562 + antagonist

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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Michal Harel, Alexander Berchansky, Nina Clavio, Joel L. Sussman

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