Selective inhibition of MDR1 P-glycoprotein-mediated transport by the acridone carboxamide derivative GG918
1999
Inhibition of Multidrug Resistance by GG918
publication
Evidence: high
Author Information
Author(s): Wallstab A, Koester M, Böhme M, Keppler D
Primary Institution: Division of Tumor Biochemistry, Deutsches Krebsforschungszentrum, Heidelberg, Germany
Hypothesis
GG918 is a potent inhibitor of MDR1 P-glycoprotein-mediated multidrug resistance.
Conclusion
GG918 effectively inhibits MDR1 P-glycoprotein-mediated transport, demonstrating high potency and selectivity.
Supporting Evidence
- GG918 showed 50% inhibition of MDR1 P-glycoprotein-mediated transport at concentrations between 8 nM and 80 nM.
- The inhibition constant Ki for GG918 was determined to be 35 nM.
- Almost complete inhibition of [3H]daunorubicin transport was observed at concentrations of GG918 that did not affect other export pumps.
Takeaway
GG918 is a special chemical that helps stop cancer cells from resisting treatment by blocking a specific protein.
Methodology
Direct measurements of ATP-dependent MDR1 P-glycoprotein-mediated transport in plasma membrane vesicles from human and rat hepatocyte canalicular membranes.
Digital Object Identifier (DOI)
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