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Inhibitors of P-Glycoprotein - Lead Identification and Optimisation

[ Vol. 5 , Issue. 2 ]


Karin Pleban and Gerhard F. Ecker   Pages 153 - 163 ( 11 )


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 Pglycoprotein.


inhibitors of p-glycoprotein, multidrug resistance, qsar, pharmacophore models


Department of Pharmaceutical Chemistry, University of Vienna, Althanstrasse 14, 1090 Wien, Austria.

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