Inhibitors of P-Glycoprotein - Lead Identification and Optimisation

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

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 5 , Issue 2 , 2005


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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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Article Details

VOLUME: 5
ISSUE: 2
Year: 2005
Page: [153 - 163]
Pages: 11
DOI: 10.2174/1389557053402729
Price: $65

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