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Ivermectin Interacts With Human ABCG2

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Presentation on theme: "Ivermectin Interacts With Human ABCG2"— Presentation transcript:

1 Ivermectin Interacts With Human ABCG2
Márton Jani, Ildikó Makai, Emese Kis, Pál Szabó, Tünde Nagy, Péter Krajcsi, Anne Lespine  Journal of Pharmaceutical Sciences  Volume 100, Issue 1, Pages (January 2011) DOI: /jps.22262 Copyright © 2010 Wiley-Liss, Inc. Terms and Conditions

2 Figure 1 Ivermectin inhibits ABCG2 function in membrane vesicles and in cells. Ivermectin was incubated at final concentrations indicated with membrane vesicles (A) or cells (B) overexpressing human ABCG2. Transport of 3H-E3S (A) or Hoechst33342 (B) was measured and inhibition of transport is shown. Data points represent arithmetic means with standard deviations of three replicates. Journal of Pharmaceutical Sciences  , 94-97DOI: ( /jps.22262) Copyright © 2010 Wiley-Liss, Inc. Terms and Conditions

3 Figure 2 Effect of ivermectin on ABCG2 ATPase. Membrane vesicles (20µg/well) were incubated with indicated concentrations of ivermectin for 40min at 32°C. The sodium orthovanadate sensitive activity was plotted. Data points represent arithmetic means with standard deviations of three replicates. Journal of Pharmaceutical Sciences  , 94-97DOI: ( /jps.22262) Copyright © 2010 Wiley-Liss, Inc. Terms and Conditions

4 Figure 3 Inhibition of BCRP-mediated E3S transport by ivermectin in Dixon's representation. Linear portion of ivermectin series is shown. E3S concentrations were 50, 16.7, 5.56, and 1.85µM. The intersections yield a Ki of 1.4µM. Journal of Pharmaceutical Sciences  , 94-97DOI: ( /jps.22262) Copyright © 2010 Wiley-Liss, Inc. Terms and Conditions

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