Title : Kinetics of anthracycline efflux from multidrug resistance protein-expressing cancer cells compared with P-glycoprotein-expressing cancer cells.

Pub. Date : 1998 Jan

PMID : 9443942






6 Functional Relationships(s)
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1 Kinetics of anthracycline efflux from multidrug resistance protein-expressing cancer cells compared with P-glycoprotein-expressing cancer cells. Anthracyclines ATP binding cassette subfamily C member 1 Homo sapiens
2 The substrate specificity of both transporter proteins is partly overlapping but is otherwise very distinct; because MRP is a multiple organic anion transporter, it transports certain glutathione conjugates and may be partly dependent on intracellular glutathione levels for the transport of anthracyclines. Anthracyclines ATP binding cassette subfamily C member 1 Homo sapiens
3 We have studied the transport kinetics of a series of anthracyclines in MRP and Pgp that overexpress tumor cell lines to obtain information on the substrate specificity of these proteins. Anthracyclines ATP binding cassette subfamily C member 1 Homo sapiens
4 Two anthracyclines, the doxorubicin derivative pirarubicin and 2"-bromo-4"-epi-DNR seemed to have a slightly higher Ka value for Pgp than for MRP. Anthracyclines ATP binding cassette subfamily C member 1 Homo sapiens
5 Determination of the Hill coefficient (nH) of the MRP-mediated efflux gave most values close to 2, which suggests cooperativity of the transport of anthracyclines as reported before for Pgp. Anthracyclines ATP binding cassette subfamily C member 1 Homo sapiens
6 In conclusion, the transport kinetics of anthracyclines by MRP and Pgp are very similar. Anthracyclines ATP binding cassette subfamily C member 1 Homo sapiens