Inhibitory effect of the reversal agents V-104, GF120918 and Pluronic L61 on MDR1 Pgp-, MRP1- and MRP2-mediated transport
2000
Effects of Reversal Agents on Drug Resistance in Cancer Cells
Sample size: 2008
publication
Evidence: moderate
Author Information
Author(s): Evers R, Kool M, Smith A J, Deemter L van, Haas M de, Borst P
Primary Institution: The Netherlands Cancer Institute
Hypothesis
Can reversal agents effectively inhibit multidrug transporters to overcome drug resistance in tumor cells?
Conclusion
The study found that V-104 effectively inhibits MDR1 Pgp and partially inhibits MRP1, while GF120918 does not reverse MRP1 resistance.
Supporting Evidence
- V-104 efficiently inhibits MDR1 Pgp.
- V-104 partially inhibits daunorubicin transport by MRP1.
- GF120918 does not reverse resistance due to MRP1.
- Pluronic L61 stimulates the export of calcein by MRP1 and MRP2 cells.
Takeaway
This study looked at how certain drugs can help fight cancer by blocking the transporters that make cancer cells resistant to treatment.
Methodology
The study used polarized cell lines expressing human MDR1, MRP1, and MRP2 to test the effects of reversal agents on drug transport.
Digital Object Identifier (DOI)
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