Potent Non-Competitive Inhibitor of the ATP-binding Cassette Multidrug Resistance Transporter ABCB1

نویسندگان

  • Gisela Caceres
  • Robert W. Robey
  • Lubomir Sokol
  • Kathy L. McGraw
  • Justine Clark
  • Nicholas J. Lawrence
  • Said M. Sebti
  • Michael Wiese
  • Alan F. List
چکیده

Running Title: HG-829, A Novel Pgp Inhibitor

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

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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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تاریخ انتشار 2012