Ivermectin Interacts With Human ABCG2

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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 94-97 (January 2011) DOI: 10.1002/jps.22262 Copyright © 2010 Wiley-Liss, Inc. Terms and Conditions

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 2011 100, 94-97DOI: (10.1002/jps.22262) Copyright © 2010 Wiley-Liss, Inc. Terms and Conditions

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 2011 100, 94-97DOI: (10.1002/jps.22262) Copyright © 2010 Wiley-Liss, Inc. Terms and Conditions

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 2011 100, 94-97DOI: (10.1002/jps.22262) Copyright © 2010 Wiley-Liss, Inc. Terms and Conditions