Overcoming multidrug drug resistance in P-glycoprotein/MDR1-overexpressing cell lines by ecteinascidin 743.

@article{Kanzaki2002OvercomingMD,
  title={Overcoming multidrug drug resistance in P-glycoprotein/MDR1-overexpressing cell lines by ecteinascidin 743.},
  author={Atsuko Kanzaki and Yuji Takebayashi and X Ren and Hitoshi Miyashita and Shiro Mori and Shin-ichi Akiyama and Yves Pommier},
  journal={Molecular cancer therapeutics},
  year={2002},
  volume={1 14},
  pages={1327-34}
}
Ecteinascidin 743 (Et-743) is a novel anticancer agent forming covalent guanine adducts at specific sites in the DNA minor groove. Et-743 has a unique mechanism of action because it kills cancer cells by poisoning transcription-coupled nucleotide excision repair. Recent studies suggested a complex relationship between P-glycoprotein (P-gp)/MDR1 and Et-743. On one hand, Et-743 was reported to down-regulate the MDR1 promoter in vitro. On the other hand, P-gp overexpression was hypothesized to… CONTINUE READING
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