Targeting adenosine receptors for the treatment of cardiac fibrosis

Elizabeth A Vecchio, Paul J White, Lauren T May

Research output: Contribution to journalReview ArticleOtherpeer-review

Abstract

Adenosine is a ubiquitous molecule with key regulatory and cytoprotective mechanisms at times of metabolic imbalance in the body. Among a plethora of physiological actions, adenosine has an important role in attenuating ischaemia-reperfusion injury and modulating the ensuing fibrosis and tissue remodeling following myocardial damage. Adenosine exerts these actions through interaction with four adenosine G protein-coupled receptors expressed in the heart. The adenosine A2B receptor (A2BAR) is the most abundant adenosine receptor (AR) in cardiac fibroblasts and is largely responsible for the influence of adenosine on cardiac fibrosis. In vitro and in vivo studies demonstrate that acute A2BAR stimulation can decrease fibrosis through the inhibition of fibroblast proliferation and reduction in collagen synthesis. However, in contrast, there is also evidence that chronic A2BAR antagonism reduces tissue fibrosis. This review explores the opposing pro- and anti-fibrotic activity attributed to the activation of cardiac ARs and investigates the therapeutic potential of targeting ARs for the treatment of cardiac fibrosis.

Original languageEnglish
Article number243
Number of pages7
JournalFrontiers in Pharmacology
Volume8
Issue numberMAY
DOIs
Publication statusPublished - 5 May 2017

Keywords

  • Adenosine
  • Adenosine A2B receptor
  • CAMP
  • Cardiac fibrosis
  • Collagen synthesis
  • Fibroblast
  • Heart failure
  • Myocardial infarction

Cite this

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Targeting adenosine receptors for the treatment of cardiac fibrosis. / Vecchio, Elizabeth A; White, Paul J; May, Lauren T.

In: Frontiers in Pharmacology, Vol. 8, No. MAY, 243, 05.05.2017.

Research output: Contribution to journalReview ArticleOtherpeer-review

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AU - White, Paul J

AU - May, Lauren T

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KW - Adenosine

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KW - Cardiac fibrosis

KW - Collagen synthesis

KW - Fibroblast

KW - Heart failure

KW - Myocardial infarction

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