Title : Folates provoke cellular efflux and drug resistance of substrates of the multidrug resistance protein 1 (MRP1).

Pub. Date : 2014 May

PMID : 24595806






13 Functional Relationships(s)
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Compound Name
Protein Name
Organism
1 Folates provoke cellular efflux and drug resistance of substrates of the multidrug resistance protein 1 (MRP1). Folic Acid ATP binding cassette subfamily B member 1 Homo sapiens
2 Folates provoke cellular efflux and drug resistance of substrates of the multidrug resistance protein 1 (MRP1). Folic Acid ATP binding cassette subfamily B member 1 Homo sapiens
3 Cellular folate concentration was earlier reported to be a critical factor in the activity and expression of the multidrug resistance protein MRP1 (ABCC1). Folic Acid ATP binding cassette subfamily B member 1 Homo sapiens
4 Since MRP1 mediates resistance to a variety of therapeutic drugs, we investigated whether the cellular folate concentration influences the MRP1-mediated cellular resistance against drugs. Folic Acid ATP binding cassette subfamily B member 1 Homo sapiens
5 In folate-deprived 2008/MRP1 cells, the MRP1-mediated efflux of its model substrate calcein decreased to ~55 % of the initial efflux rate under folate-rich conditions. Folic Acid ATP binding cassette subfamily B member 1 Homo sapiens
6 In folate-deprived 2008/MRP1 cells, the MRP1-mediated efflux of its model substrate calcein decreased to ~55 % of the initial efflux rate under folate-rich conditions. Folic Acid ATP binding cassette subfamily B member 1 Homo sapiens
7 In folate-deprived 2008/MRP1 cells, the MRP1-mediated efflux of its model substrate calcein decreased to ~55 % of the initial efflux rate under folate-rich conditions. Folic Acid ATP binding cassette subfamily B member 1 Homo sapiens
8 In folate-deprived 2008/MRP1 cells, the MRP1-mediated efflux of its model substrate calcein decreased to ~55 % of the initial efflux rate under folate-rich conditions. Folic Acid ATP binding cassette subfamily B member 1 Homo sapiens
9 Folate depletion for 5-10 days markedly increased (~500 %) cellular steady-state accumulation of calcein in 2008/MRP1 cells and moderately in 2008wt cells. Folic Acid ATP binding cassette subfamily B member 1 Homo sapiens
10 Folate deprivation markedly increased growth inhibitory effects of the established MRP1 substrates daunorubicin (~twofold), doxorubicin (~fivefold), and methotrexate (~83-fold) in MRP1-overexpressing cells, proportional to MRP1 expression. Folic Acid ATP binding cassette subfamily B member 1 Homo sapiens
11 Folate deprivation markedly increased growth inhibitory effects of the established MRP1 substrates daunorubicin (~twofold), doxorubicin (~fivefold), and methotrexate (~83-fold) in MRP1-overexpressing cells, proportional to MRP1 expression. Folic Acid ATP binding cassette subfamily B member 1 Homo sapiens
12 Folate deprivation markedly increased growth inhibitory effects of the established MRP1 substrates daunorubicin (~twofold), doxorubicin (~fivefold), and methotrexate (~83-fold) in MRP1-overexpressing cells, proportional to MRP1 expression. Folic Acid ATP binding cassette subfamily B member 1 Homo sapiens
13 In conclusion, this study demonstrates that increased cellular folate concentrations induce MRP1/ABCC1-related drug efflux and drug resistance. Folic Acid ATP binding cassette subfamily B member 1 Homo sapiens