Submit Manuscript  

Article Details


Inhibitors of P-Glycoprotein - Lead Identification and Optimisation

[ Vol. 5 , Issue. 2 ]

Author(s):

Karin Pleban and Gerhard F. Ecker   Pages 153 - 163 ( 11 )

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

Affiliation:

Department of Pharmaceutical Chemistry, University of Vienna, Althanstrasse 14, 1090 Wien, Austria.



Read Full-Text article