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Mini-Reviews in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Inhibitors of P-Glycoprotein - Lead Identification and Optimisation

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

Volume 5, Issue 2, 2005

Page: [153 - 163] Pages: 11

DOI: 10.2174/1389557053402729

Price: $65

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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