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
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
Affiliation:
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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Cite this article as:
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
DOI https://dx.doi.org/10.2174/1389557053402729 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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