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Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation

Overview of attention for article published in Journal of Inflammation, November 2014
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Title
Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation
Published in
Journal of Inflammation, November 2014
DOI 10.1186/s12950-014-0037-0
Pubmed ID
Authors

Ajith A Welihinda, Edward P Amento

Abstract

Adenosine is produced at high levels at inflamed sites as a by-product of cellular activation and breakdown. Adenosine mediates its anti-inflammatory activity primarily through the adenosine A2a receptor (A2aR), a member of the G-protein coupled receptors. A2aR agonists have demonstrated anti-inflammatory efficacy, however, their therapeutic utility is hindered by a lack of adenosine receptor subtype selectivity upon systemic exposure. We sought to harness the anti-inflammatory effects of adenosine by enhancing the responsiveness of A2aR to endogenously produced adenosine through allosteric modulation. We have identified a family of positive allosteric modulators (PAMs) of the A2aR. Using one member of this PAM family, AEA061, we demonstrate that A2aRs are amenable to allosteric enhancement and such enhancement produces increased A2aR signaling and diminished inflammation in vivo.

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X Demographics

The data shown below were collected from the profile of 1 X user who shared this research output. Click here to find out more about how the information was compiled.
Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 30 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 30 100%

Demographic breakdown

Readers by professional status Count As %
Researcher 10 33%
Student > Bachelor 5 17%
Student > Ph. D. Student 4 13%
Student > Master 3 10%
Student > Doctoral Student 2 7%
Other 2 7%
Unknown 4 13%
Readers by discipline Count As %
Biochemistry, Genetics and Molecular Biology 7 23%
Agricultural and Biological Sciences 5 17%
Pharmacology, Toxicology and Pharmaceutical Science 4 13%
Medicine and Dentistry 4 13%
Chemistry 3 10%
Other 2 7%
Unknown 5 17%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 05 December 2014.
All research outputs
#22,759,452
of 25,374,647 outputs
Outputs from Journal of Inflammation
#393
of 425 outputs
Outputs of similar age
#315,564
of 369,460 outputs
Outputs of similar age from Journal of Inflammation
#7
of 8 outputs
Altmetric has tracked 25,374,647 research outputs across all sources so far. This one is in the 1st percentile – i.e., 1% of other outputs scored the same or lower than it.
So far Altmetric has tracked 425 research outputs from this source. They receive a mean Attention Score of 4.9. This one is in the 1st percentile – i.e., 1% of its peers scored the same or lower than it.
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We're also able to compare this research output to 8 others from the same source and published within six weeks on either side of this one.