Inhibitors of p-glycoprotein--lead identification and optimisation.

  title={Inhibitors of p-glycoprotein--lead identification and optimisation.},
  author={Karin Pleban and Gerhard F. Ecker},
  journal={Mini reviews in medicinal chemistry},
  volume={5 2},
The membrane bound drug efflux pump P-glycoprotein (P-gp) transports a wide variety of functionally and structurally diverse cytotoxic drugs out of tumour cells. Overexpression of P-glycoprotein is one of the predominant mechanisms responsible for development of multiple drug resistance in tumour therapy. Thus, inhibition of P-gp represents a promising approach for treatment of multidrug resistant tumours. This review highlights concepts for identification and optimization of new inhibitors of… CONTINUE READING

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