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Quinoline carboxamides as modulators of Breast Cancer Resistance Protein (ABCG2): Investigations on potency, selectivity, mechanism of action, cytotoxicity, stability and drug-like properties

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Bauer, Stefanie
Date of publication of this fulltext: 12 Mar 2014 12:30

Abstract (English)

Multidrug transporter proteins such as ABCB1, ABCC1 and ABCG2 are known to contribute the chemoresistance of malignant tumors. Expression of these transporters by cancer cells leads to an efflux of anticancer drugs. The inhibition of efflux pumps, namely ABCB1, has been explored in clinical trials to overcome ABC transporter mediated drug resistance in cancer patients, but did not lead to a drug ...


Translation of the abstract (German)

ABC Transporter wie ABCB1, ABCC1 und ABCG2 tragen wesentlich zur Ausbildung von Chemoresistenzen maligner Tumore bei. Zahlreiche therapeutisch relevante Zytostatika sind Substrate dieser Transporter. Die Expression der Transporter in der Membran von Krebszellen führt zu einem verstärkten Efflux der entsprechenden Wirkstoffe und bedingt den Phänotyp der Multidrug Resistenz, was die Effektivität ...


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