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VCU Massey Cancer Center researchers identify a new class of anti-cancer drugs based on platinum

nd was designed to overcome resistance by emphasizing new modes of DNA binding, and in the process we have found that the amount of platinum drug entering cells is increased," he said. "The effectiveness of a platinum drug in killing cells is directly related to its concentration inside the cell."

DNA-damaging agents, such as cisplatin, are among the most effective classes of compounds in clinical use for the treatment of cancer. The principal function of cisplatin is to bind to DNA. Platinum drugs are the largest class of anti-cancer drugs in the clinic and the most important in terms of treatment. Cisplatin is a chemotherapy drug that is given for the treatment of metastatic testicular or ovarian cancers, and some advanced bladder cancer, and is a very effective drug in combination with other therapies.

However, according to Farrell, these current agents have limited activity against many common human cancers, and they are susceptible to acquired drug resistance. He added that resistance to cisplatin has become a clinically relevant issue ?especially for patients battling ovarian cancer because they develop resistance to cisplatin at a rapid rate.

Farrell said that use of the "non-covalent" approach and emphasizing cell uptake may help minimize the side effects of current platinum drugs. He said that both cell uptake and the ability of the cell to minimize the effect of DNA attack, or DNA repair, play a critical role in cellular resistance to cisplatin by altering its ability to effectively kill tumor cells. By understanding the features of cisplatin that contribute to resistance, Farrell and his team designed the new compound to circumvent these problems.


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Source:Virginia Commonwealth University


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