NDLI: Adenosine receptors as drug targets--what are the challenges?

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Adenosine receptors as drug targets--what are the challenges?

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Chen, Jiang-Fan Eltzschig, Holger K. Fredholm, Bertil B.
Spatial Coverage	United States
Description	Country affiliation: United States Author Affiliation: Chen JF ( Department of Neurology and Pharmacology, Boston University School of Medicine, Boston, Massachusetts 02118, USA.)
Abstract	Adenosine signalling has long been a target for drug development, with adenosine itself or its derivatives being used clinically since the 1940s. In addition, methylxanthines such as caffeine have profound biological effects as antagonists at adenosine receptors. Moreover, drugs such as dipyridamole and methotrexate act by enhancing the activation of adenosine receptors. There is strong evidence that adenosine has a functional role in many diseases, and several pharmacological compounds specifically targeting individual adenosine receptors--either directly or indirectly--have now entered the clinic. However, only one adenosine receptor-specific agent--the adenosine A2A receptor agonist regadenoson (Lexiscan; Astellas Pharma)--has so far gained approval from the US Food and Drug Administration (FDA). Here, we focus on the biology of adenosine signalling to identify hurdles in the development of additional pharmacological compounds targeting adenosine receptors and discuss strategies to overcome these challenges.
File Format	HTM / HTML
ISSN	14741776
e-ISSN	14741784
DOI	10.1038/nrd3955
Journal	Nature Reviews Drug Discovery
Issue Number	4
Volume Number	12
Language	English
Publisher	Nature Publishing Group
Publisher Date	2013-04-01
Publisher Place	Great Britain (UK)
Access Restriction	Open
Subject Keyword	Discipline Pharmacology Discipline Biotechnology Drug Design Molecular Targeted Therapy Receptors, Purinergic P1 Drug Effects Adenosine A2 Receptor Agonists Pharmacology Animals Drug Approval Purines Pyrazoles Metabolism Signal Transduction United States Food And Drug Administration Research Support, N.i.h., Extramural Research Support, Non-u.s. Gov't
Content Type	Text
Resource Type	Article
Subject	Medicine Drug Discovery Pharmacology

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