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Current Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Towards Next Generation Adenosine A2A Receptor Antagonists

Author(s): G. Yuan and G.B. Jones

Volume 21, Issue 34, 2014

Page: [3918 - 3935] Pages: 18

DOI: 10.2174/0929867321666140826115123

Price: $65

Abstract

The Adenosine A2A receptor is a member of the G-protein coupled receptor superfamily. It plays a key role in numerous physiological processes through the central nervous system and in peripheral tissues. Functional interactions between the A2A and dopamine D2 receptor has spurred interest in the use of antagonists as anti-Parkinson drugs. Additionally, oncology drugs are now being designed based on the potential for A2A antagonists to function as immunotherapeutics. From early studies based on classical xanthine type A2A antagonists through second generation agents, this mini review will cover aspects of the discovery, development, chemical synthesis and medicinal evaluation of this important class of drugs.

Keywords: A2AR antagonists, aqueous solubility, cancer immunotherapy, molecular modeling, parkinson's disease, PET imaging, X-ray crystallography.


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