Is the adenosine A2B 'biased' receptor a valuable target for the treatment of pulmonary arterial hypertension?

Drug Discov Today. 2018 Jun;23(6):1285-1292. doi: 10.1016/j.drudis.2018.05.005. Epub 2018 May 7.

Abstract

Pulmonary arterial hypertension (PAH) is a maladaptive disorder characterized by increased pulmonary vascular resistance leading to right ventricular failure and death. Adenosine released by injured tissues, such as the lung and heart, influences tissue remodeling through the activation of adenosine receptors. Evidence regarding activation of the low-affinity A2BAR by adenosine points towards pivotal roles of this receptor in processes associated with both acute and chronic lung diseases. Conflicting results exist concerning the beneficial or detrimental roles of the A2B 'biased' receptor in right ventricular failure secondary to PAH. In this review, we discuss the pros and cons of manipulating A2BARs as a putative therapeutic target in PAH.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Biological Transport
  • Cell Membrane
  • Humans
  • Hypertension, Pulmonary / drug therapy*
  • Hypertension, Pulmonary / metabolism
  • Ligands
  • Lung / blood supply
  • Lung / metabolism
  • Myocardium / metabolism
  • Receptor, Adenosine A2B / metabolism*
  • Signal Transduction

Substances

  • Ligands
  • Receptor, Adenosine A2B