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  • Title: Inhibitors of p-glycoprotein--lead identification and optimisation.
    Author: Pleban K, Ecker GF.
    Journal: Mini Rev Med Chem; 2005 Feb; 5(2):153-63. PubMed ID: 15720285.
    Abstract:
    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 P-glycoprotein.
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