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  • ATP-binding drug efflux transporters decrease intracellular concentrations of cytotoxic drugs, causing multidrug resistance in cancer. In this study, we examined possible interactions of ABCG2 transporter with platinum cytotoxic drugs. We demonstrate here an interference of platinum drugs with enhanced green fluorescence protein (EGFP) in the cellular models, where EGFP was employed as a reporter gene. Cytotoxicity of cisplatin (CIP), carboplatin (CAP) and oxaliplatin (OXP) was significantly lowered in MDCKII cells transfected with ABCG2 transporter and EGFP reporter. The IC(50) values in MDCKII-ABCG2 were 25.7, 164 and 165 microM for CIP, CAP and OXP, respectively, whereas IC(50) for the same cytostatics in MDCKII cells were as follows: 15.4, 133 and 50.3 microM. Addition of fumitremorgin C (FTC), a potent ABCG2 inhibitor, significantly suppressed the resistance of MDCKII-ABCG2 to OXP, suggesting that OXP interacts with ABCG2. However, FTC did not change the sensitivity of the cells to CIP and CAP.
  • ATP-binding drug efflux transporters decrease intracellular concentrations of cytotoxic drugs, causing multidrug resistance in cancer. In this study, we examined possible interactions of ABCG2 transporter with platinum cytotoxic drugs. We demonstrate here an interference of platinum drugs with enhanced green fluorescence protein (EGFP) in the cellular models, where EGFP was employed as a reporter gene. Cytotoxicity of cisplatin (CIP), carboplatin (CAP) and oxaliplatin (OXP) was significantly lowered in MDCKII cells transfected with ABCG2 transporter and EGFP reporter. The IC(50) values in MDCKII-ABCG2 were 25.7, 164 and 165 microM for CIP, CAP and OXP, respectively, whereas IC(50) for the same cytostatics in MDCKII cells were as follows: 15.4, 133 and 50.3 microM. Addition of fumitremorgin C (FTC), a potent ABCG2 inhibitor, significantly suppressed the resistance of MDCKII-ABCG2 to OXP, suggesting that OXP interacts with ABCG2. However, FTC did not change the sensitivity of the cells to CIP and CAP. (en)
Title
  • Effect of ABCG2 on cytotoxicity of platinum drugs: Interference of EGFP
  • Effect of ABCG2 on cytotoxicity of platinum drugs: Interference of EGFP (en)
skos:prefLabel
  • Effect of ABCG2 on cytotoxicity of platinum drugs: Interference of EGFP
  • Effect of ABCG2 on cytotoxicity of platinum drugs: Interference of EGFP (en)
skos:notation
  • RIV/63221667:_____/08:#0000022!RIV10-MZ0-63221667
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • P(1A8696), S
http://linked.open...iv/cisloPeriodika
  • 8
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
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  • 364985
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  • RIV/63221667:_____/08:#0000022
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  • Platinum cytostatics; ABCG2; MTT assay; Neutral red assay; Cytotoxicity; Apoptosis; EGFP (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • NL - Nizozemsko
http://linked.open...ontrolniKodProRIV
  • [C31E48F860D2]
http://linked.open...i/riv/nazevZdroje
  • Toxicology in Vitro
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http://linked.open...vavai/riv/projekt
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 22
http://linked.open...iv/tvurceVysledku
  • Čečková, Martina
  • Štaud, František
  • Bunček, Martin
  • Libra, Antonín
  • Vacková, Zuzana
  • Radilová, Hana
issn
  • 0887-2333
number of pages
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