Title : MDR1 causes resistance to the antitumour drug miltefosine.

Pub. Date : 2001 May 18

PMID : 11355955






10 Functional Relationships(s)
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Compound Name
Protein Name
Organism
1 MDR1 causes resistance to the antitumour drug miltefosine. miltefosine ATP binding cassette subfamily B member 1 Homo sapiens
2 We investigated the sensitivity of MDR1 -expressing cells to treatment with miltefosine. miltefosine ATP binding cassette subfamily B member 1 Homo sapiens
3 We show that cells overexpressing MDR1 (NCI/ADR-RES, KB-8-5, KB-C1, CCRF/VCR1000, CCRF/ADR5000) were less sensitive to miltefosine treatment when compared to the sensitive parental cell lines. miltefosine ATP binding cassette subfamily B member 1 Homo sapiens
4 HeLa cells transfected with MDR1 exhibited resistance to the compound, indicating that expression of this gene is sufficient to reduce the sensitivity to miltefosine. miltefosine ATP binding cassette subfamily B member 1 Homo sapiens
5 The resistance of MDR1-expressing cells to miltefosine was less pronounced than that to adriamycin or vinblastine. miltefosine ATP binding cassette subfamily B member 1 Homo sapiens
6 As shown by a fluorescence quenching assay using MIANS-labelled P-glycoprotein (PGP), miltefosine bound to PGP with a K(d)of approximately 7 microM and inhibited PGP-ATPase activity with an IC(50)of approximately 35 microM. miltefosine ATP binding cassette subfamily B member 1 Homo sapiens
7 As shown by a fluorescence quenching assay using MIANS-labelled P-glycoprotein (PGP), miltefosine bound to PGP with a K(d)of approximately 7 microM and inhibited PGP-ATPase activity with an IC(50)of approximately 35 microM. miltefosine ATP binding cassette subfamily B member 1 Homo sapiens
8 As shown by a fluorescence quenching assay using MIANS-labelled P-glycoprotein (PGP), miltefosine bound to PGP with a K(d)of approximately 7 microM and inhibited PGP-ATPase activity with an IC(50)of approximately 35 microM. miltefosine ATP binding cassette subfamily B member 1 Homo sapiens
9 As shown by a fluorescence quenching assay using MIANS-labelled P-glycoprotein (PGP), miltefosine bound to PGP with a K(d)of approximately 7 microM and inhibited PGP-ATPase activity with an IC(50)of approximately 35 microM. miltefosine ATP binding cassette subfamily B member 1 Homo sapiens
10 These data indicate that expression of MDR1 may reduce the response to miltefosine in patients and that this compound interacts with PGP in a manner different from a number of other substrates. miltefosine ATP binding cassette subfamily B member 1 Homo sapiens