Inhibitors of P-Glycoprotein - Lead Identification and Optimisation

Karin      Pleban; Gerhard   F.   Ecker

doi:10.2174/1389557053402729

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 Pglycoprotein.

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

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Mini-Reviews in Medicinal Chemistry

Title: Inhibitors of P-Glycoprotein - Lead Identification and Optimisation

Volume: 5 Issue: 2

Author(s): Karin Pleban and Gerhard F. Ecker

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

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 Pglycoprotein.

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Pleban Karin and Ecker F. Gerhard, Inhibitors of P-Glycoprotein - Lead Identification and Optimisation, Mini-Reviews in Medicinal Chemistry 2005; 5 (2) . https://dx.doi.org/10.2174/1389557053402729