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Adenosine receptors as therapeutic targets
Kenneth A Jacobson1, Zhan-Guo Gao
1Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes, Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892-0810, USA. kajacobs@helix.nih.gov
Caffeine targets adenosine receptors, which are also promising for treating various diseases like cancer and sleep disorders. Recent advances in selective ligands bring therapeutic applications closer.
Area of Science:
- Pharmacology
- Medicinal Chemistry
- Neuroscience
Background:
- Adenosine receptors are key targets for caffeine, a widely consumed drug.
- Emerging evidence suggests their therapeutic potential in conditions including ischaemic diseases, sleep disorders, immune disorders, and cancer.
Purpose of the Study:
- To review recent advances in understanding adenosine receptor subtypes.
- To discuss the development of selective ligands for therapeutic applications.
Main Methods:
- Medicinal chemistry research over three decades.
- Discovery and clinical evaluation of adenosine receptor agonists and antagonists.
- Review of recent scientific literature on adenosine receptor modulators.
Main Results:
- Numerous selective adenosine receptor agonists and antagonists have been identified.
- Some developed ligands have undergone clinical evaluation.
- Understanding of adenosine receptor subtype roles has advanced significantly.
Conclusions:
- Despite no current regulatory approvals, therapeutic applications of adenosine receptor modulators are closer.
- Advances in selective ligand development and understanding of receptor subtypes are driving progress.
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