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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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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|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|
|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
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Yes|
|Deposited On:||14 Jan 2009 11:03|
|Last Modified:||08 Nov 2010 10:18|