HG-829 Is a Potent Noncompetitive Inhibitor of the ATP-Binding Cassette Multidrug Resistance Transporter ABCB1

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HG-829 is a potent noncompetitive inhibitor of the ATP-binding cassette multidrug resistance transporter ABCB1.

Transmembrane drug export mediated by the ATP-binding cassette (ABC) transporter P-glycoprotein contributes to clinical resistance to antineoplastics. In this study, we identified the substituted quinoline HG-829 as a novel, noncompetitive, and potent P-glycoprotein inhibitor that overcomes in vitro and in vivo drug resistance. We found that nontoxic concentrations of HG-829 restored sensitivit...

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Therapeutics, Targets, and Chemical Biology HG-829 Is a Potent Noncompetitive Inhibitor of the ATP- Binding Cassette Multidrug Resistance Transporter ABCB1

Transmembrane drug export mediated by the ATP-binding cassette (ABC) transporter P-glycoprotein contributes to clinical resistance to antineoplastics. In this study, we identified the substituted quinoline HG-829 as a novel, noncompetitive, and potent P-glycoprotein inhibitor that overcomes in vitro and in vivo drug resistance. We found that nontoxic concentrations of HG-829 restored sensitivit...

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The role of ATP-binding cassette transporter A2 in childhood acute lymphoblastic leukemia multidrug resistance

Acute lymphoblastic leukemia (ALL) is one of the most prevalent hematologic malignancies in children. Although the cure rate of ALL has improved over the past decades, the most important reason for ALL treatment failure is multidrug resistance (MDR) phenomenon. The current study aims to explain the mechanisms involved in multidrug resistance of childhood ALL, and introduces ATP-binding cassette...

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the role of atp-binding cassette transporter a2 in childhood acute lymphoblastic leukemia multidrug resistance

acute lymphoblastic leukemia (all) is one of the most prevalent hematologic malignancies in children. although the cure rate of all has improved over the past decades, the most important reason for all treatment failure is multidrug resistance (mdr) phenomenon. the current study aims to explain the mechanisms involved in multidrug resistance of childhood all, and introduces atp-binding cassette...

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ژورنال

عنوان ژورنال: Cancer Research

سال: 2012

ISSN: 0008-5472,1538-7445

DOI: 10.1158/0008-5472.can-12-0743