title: Turning tumor-promoting copper into an anti-cancer weapon via high-throughput chemistry.
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.
authors.affiliation: Shandong University, Jinan, China.
authors.forename: F
authors.initials: F
authors.lastname: Wang
authors.forename: P
authors.initials: P
authors.lastname: Jiao
authors.forename: M
authors.initials: M
authors.lastname: Qi
authors.forename: M
authors.initials: M
authors.lastname: Frezza
authors.forename: Q P
authors.initials: QP
authors.lastname: Dou
authors.forename: B
authors.initials: B
authors.lastname: Yan
mesh_terms: D043925:Angiogenesis Inducing Agents / Q000378:metabolism*; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002273:Carcinogens / Q000378:metabolism*; D002614:Chelating Agents / Q000494:pharmacology; D003300:Copper / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D057166:High-Throughput Screening Assays / Q000379:methods*; D006801:Humans; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy*; D018384:Oxidative Stress / Q000502:physiology; D011480:Protease Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D046988:Proteasome Endopeptidase Complex / Q000494:pharmacology; D051381:Rats; D017382:Reactive Oxygen Species / Q000737:chemistry / Q000494:pharmacology
chemical_list: D043925:Angiogenesis Inducing Agents; D000970:Antineoplastic Agents; D002273:Carcinogens; D002614:Chelating Agents; D011480:Protease Inhibitors; D017382:Reactive Oxygen Species; D003300:Copper; D046988:Proteasome Endopeptidase Complex