Evaluation and comparison of MRP1 activity with three fluorescent dyes and three modulators in leukemic cell lines

MRP1 activity was evaluated and compared in 11 cell lines with different levels of MRP1 expression using functional assays of calcein acetoxymethyl ester (calcein-AM), carboxyfluorescein diacetate (CFDA) and Rhodamine 123 (Rh123) in combination with the modulators cyclosporin A (CsA), probenecid and...

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Veröffentlicht in:	Leukemia research 2004-06, Vol.28 (6), p.619-622
Hauptverfasser:	Dogan, A.Lale, Legrand, Ollivier, Faussat, Anne-Marie, Perrot, Jean-Yves, Marie, Jean-Pierre
Format:	Artikel
Sprache:	eng
Schlagworte:	ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism Biological Transport - drug effects Bronchodilator Agents - pharmacology Calcein-AM Carboxyfluorescein diacetate (CFDA) Cyclosporine - pharmacology Drug Resistance, Multiple Drug Resistance, Neoplasm Enzyme Inhibitors - pharmacology Fluoresceins - pharmacokinetics Fluorescent Dyes - pharmacokinetics Humans Leukemia - metabolism Leukemia - pathology MDR1 MRP1 Multidrug Resistance-Associated Proteins - metabolism Probenecid - pharmacology Propionates - pharmacology Quinolines - pharmacology Rhodamine 123 (Rh123) Rhodamine 123 - pharmacokinetics Tumor Cells, Cultured
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Zusammenfassung:	MRP1 activity was evaluated and compared in 11 cell lines with different levels of MRP1 expression using functional assays of calcein acetoxymethyl ester (calcein-AM), carboxyfluorescein diacetate (CFDA) and Rhodamine 123 (Rh123) in combination with the modulators cyclosporin A (CsA), probenecid and MK571. A good correlation was found between MRP1 expression and the modulatory effect of MK571 on calcein-AM uptake ( P=0.01) and probenecid effect on CFDA uptake ( P=0.02). Additionally, the combined modulatory effect of MK571 and probenecid on CFDA uptake ( P
ISSN:	0145-2126 1873-5835
DOI:	10.1016/j.leukres.2003.10.015