Adenosine receptor targeting in health and disease

Abstract

Introduction: The adenosine receptors A₁, A_2A, A_2B and A₃ are important and ubiquitous mediators of cellular signaling that play vital roles in protecting tissues and organs from damage. In particular, adenosine triggers tissue protection and repair by different receptor-mediated mechanisms, including increasing the oxygen supply:demand ratio, pre-conditioning, anti-inflammatory effects and the stimulation of angiogenesis.

Areas covered: The state of the art of the role of adenosine receptors which have been proposed as targets for drug design and discovery, in health and disease, and an overview of the ligands for these receptors in clinical development.

Expert opinion: Selective ligands of A₁, A_2A, A_2B and A₃ adenosine receptors are likely to find applications in the treatment of pain, ischemic conditions, glaucoma, asthma, arthritis, cancer and other disorders in which inflammation is a feature. The aim of this review is to provide an overview of the present knowledge regarding the role of these adenosine receptors in health and disease.

Keywords:

• adenosine receptors
• cancer
• cardiovascular diseases
• health
• inflammation
• neurological diseases
• respiratory disorders

Acknowledgement

S Gessi and S Merighi contributed equally to this work.

Notes

This box summarizes key points contained in the article.