Title: Turning Tumor-Promoting Copper into an Anti-Cancer Weapon via High-Throughput Chemistry
VOLUME: 17 ISSUE: 25
Author(s):F. Wang, P. Jiao, M. Qi, M. Frezza, Q.P. Dou and B. Yan
Affiliation:Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, TN, 38105, USA.
Keywords:Copper, oxidative stress, proteasome inhibitor, ROS, angiogenesis
Abstract: 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.
