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Potent and selective inhibitors of breast cancer resistance protein (ABCG2) derived from the p-glycoprotein (ABCB1) modulator tariquidar

Kühnle, Matthias and Egger, Michael and Müller, Christine and Mahringer, Anne and Bernhardt, Günther and Fricker, Gert and König, Burkhard and Buschauer, Armin (2009) Potent and selective inhibitors of breast cancer resistance protein (ABCG2) derived from the p-glycoprotein (ABCB1) modulator tariquidar. Journal of Medicinal Chemistry 52 (4), pp. 1190-1197.

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Abstract

The efflux pumps ABCB1 (p-gp, MDR1) and ABCG2 (BCRP) are expressed to a high extent by endothelial cells at the blood-brain barrier (BBB) and other barrier tissues, and are involved in drug resistance of tumor (stem) cells. Whereas numerous ABCB1 inhibitors are known, only a few ABCG2 modulators with submicromolar activity have been published. Starting from tariquidar (4) analogs as ABCB1 ...

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Item Type:Article
Date:26 January 2009
Institutions:Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König
Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Projects:GRK 760, Graduiertenkolleg Medizinische Chemie
Identification Number:
ValueType
10.1021/jm8013822DOI
19170519PubMed ID
Related URLs:
URLURL Type
http://pubs.acs.org/doi/full/10.1021/jm8013822Publisher
http://pubs.acs.org/doi/pdf/10.1021/jm8013822Publisher
http://pubs.acs.org/doi/suppl/10.1021/jm8013822/suppl_file/jm8013822_si_001.pdfSupplementary Material
Keywords:ABC transporter, BCRP, ABCG2, p-glycoprotein, ABCB1, cytotoxicity, MCF-7 breast cancer cells
Subjects:500 Science > 570 Life sciences
500 Science > 540 Chemistry & allied sciences
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Owner: Regina Hoheisel
Deposited On:14 Jan 2009 11:03
Last Modified:08 Nov 2010 10:18
Item ID:4922
Owner Only: item control page
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