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Keywords:

  • Bioinorganic chemistry;
  • ­Medicinal chemistry;
  • Drug design;
  • Drug delivery;
  • Antitumor agents;
  • Platinum;
  • Copper transport proteins

Abstract

Cisplatin, or cis-diamminedichloridoplatinum(II) cis-[PtCl2(NH3)2], is a platinum-based anticancer drug largely used for the treatment of various types of cancers, including ovarian and colorectal carcinomas, sarcomas, and lymphomas. Together with other platinum-based drugs, it triggers malignant cell death by binding to nuclear DNA, which appears to be the ultimate target. In addition to passive diffusion across the cell membrane, other transport mechanisms, including endocytosis and some active or facilitated transport, are currently proposed to play a pivotal role in the uptake of platinum-based drugs. In this microreview, we will give an updated view of the current literature regarding cisplatin transport and processing inside the cell, with special emphasis on the membrane copper transporter Ctr1 and the soluble copper chaperone Atox1.