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Current Medicinal Chemistry


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

Turning Tumor-Promoting Copper into an Anti-Cancer Weapon via High-Throughput Chemistry

Author(s): F. Wang, P. Jiao, M. Qi, M. Frezza, Q.P. Dou and B. Yan

Volume 17, Issue 25, 2010

Page: [2685 - 2698] Pages: 14

DOI: 10.2174/092986710791859315

Price: $65


Copper is an essential element for multiple biological processes. Its concentration is elevated to a very high level in cancer tissues for promoting cancer development through processes such as angiogenesis. Organic chelators of copper can passively reduce cellular copper and serve the role as inhibitors of angiogenesis. However, they can also actively attack cellular targets such as proteasome, which plays a critical role in cancer development and survival. The discovery of such molecules initially relied on a step by step synthesis followed by biological assays. Today high-throughput chemistry and high-throughput screening have significantly expedited the copper-binding molecules discovery to turn “cancer-promoting” copper into anti-cancer agents.

Keywords: Copper, oxidative stress, proteasome inhibitor, ROS, angiogenesis

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