FIGURE

Figure 1

ID
ZDB-FIG-200817-31
Publication
Creusot et al., 2020 - The Anti-Cancer Drug Dabrafenib Is a Potent Activator of the Human Pregnane X Receptor
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Figure 1

Effects of dabrafenib on the activation of human, mouse and zebrafish pregnane X receptor (PXR) and human constitutive androstane receptor (CAR) nuclear receptors as measured by luciferase reporter assay. Activation has been measured in (A) HG5LN control cells or cells expressing GAL4 fusion with (B) human (hPXR), (C) mouse (mPXR) or (D) zebrafish (zfPXR) PXR, (E) human wild-type (hCAR) or (F) mutated (hCAR APYLT) hCAR LBD treated by DMSO (0.1%), SR12813 3 μM, PCN 3 μM, clotrimazol 1 μM, CITCO 1 μM and dabrafenib 3 μM. Results are expressed as fold induction as compared to control. Data are expressed as the mean ± sd of three independent experiments, **** p < 0.0001, *** p < 0.001, ** p < 0.01 (Student’s t-test) compared with DMSO-treated cells.

Expression Data

Expression Detail
Antibody Labeling
Phenotype Data

Phenotype Detail
Acknowledgments
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