Understanding and Improving Platinum Anticancer Drugs - Phenanthriplatin
Author(s)Johnstone, Timothy; Park, Ga Young; Lippard, Stephen J.
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Approximately half of all patients who receive anticancer chemotherapy are treated with a platinum drug. Despite the widespread use of these drugs, the only cure that can be claimed is that of testicular cancer following cisplatin treatment. This article reviews some of our recent work on phenanthriplatin, a cisplatin derivative in which a chloride ion is replaced by phenanthridine, and on one of its analogues, the previously reported pyriplatin. These cationic complexes form monofunctional adducts on DNA that do not significantly distort the duplex, yet efficiently block transcription. Cell-based assays reveal altered cellular uptake properties and a cancer cell-killing profile different from those of established platinum drugs. Mechanistic work, including a crystal structure analysis of platinum-modified DNA in the active site of RNA polymerase II, is discussed herein.
DepartmentDavid H. Koch Institute for Integrative Cancer Research at MIT; Massachusetts Institute of Technology. Department of Chemistry
The International Institute of Anticancer Research
Johnstone, Timothy C., Ga Young Park, and Stephen J. Lippard. "Understanding and Improving Platinum Anticancer Drugs - Phenanthriplatin." Anticancer Research 34(1) (January 2014), 471-476.
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