Figure 2 from Systematic Evaluation of Tyrosine Kinase Inhibitors as OATP1B1 Substrates Using a Competitive Counterflow Screen

Using a biomarker and in silico docking to evaluate pazopanib as a substrate. Kinase activity of VEGFR kinase from OATP1B1-overexpressing and vector control (VC) cells (A) and hepatocytes isolated from WT and OATP1A/1B-KO mice (error bars represent SD; ***, P < 0.001; B) following a 1-hour treatment with 10 μmol/L pazopanib. Kinase activity was assessed by ADP-Glo (error bars represent SD; ****, P < 0.0001). Molecular in silico docking of pazopanib in elucidated OATP1B1 structure (C) and with E3S superimposed (D).