The specific bisindolylmaleimide PKC-inhibitor GF 109203X efficiently modulates MRP-associated multiple drug resistance.

@article{Gekeler1995TheSB,
  title={The specific bisindolylmaleimide PKC-inhibitor GF 109203X efficiently modulates MRP-associated multiple drug resistance.},
  author={Volker Gekeler and Rainer Boer and Wataru Ise and Karl H. Sanders and C. Schaechtele and Jessalyn Beck},
  journal={Biochemical and biophysical research communications},
  year={1995},
  volume={206 1},
  pages={
          119-26
        }
}
The newly identified drug transporter MRP is functionally linked to a multiple drug resistance independent from P-glycoprotein. Resistance modifiers for this type of MDR are rare at present. We analyzed the modulating effect of the highly selective bisindolylmaleimide PKC inhibitor GF 109203X on the MRP overexpressing human MDR sublines HL60/AR and GLC4/ADR. Applying a 72 hour MTT-assay we demonstrate a complete reversal of the vincristine resistance of HL60/AR cells. Adriamycin resistance of… CONTINUE READING
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