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

Become EABM
Become Reviewer
Call for Editor


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

Rights & PermissionsPrintExport Cite as

Article Details

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

Article Metrics

PDF: 4