Fig. 2: JMV7048 is a PXR degrader.
From: Targeting pregnane X receptor with a potent agonist-based PROTAC to delay colon cancer relapse
A Western blot analysis and quantification of PXR protein expression levels in LS174T cells treated with the indicated JMV7048 concentrations. Data are expressed as mean ± SD (n > 3) and normalized to untreated cells (O). B Parallel analysis of LS174T cell proliferation index (C.I., xCELLigence apparatus) and quantification of PXR mRNA and protein expression levels after treatment with 5 µM JMV7048. Data are expressed as mean ± SD (n = 3). C Cell viability analysis of LS174T cells treated for 72 h with increasing concentrations of JMV7048 or SN38. Data are expressed as mean ± SD (n = 3). D Western blot analysis and quantification of PXR protein expression in LS174T after an initial treatment of 6 h with 500 nM JMV7048 following by its removal and wash-out for different times. Data are expressed as mean ± SD (n = 3). P values are shown compared to the initial condition (B–D) data are normalized to the DMSO condition. ***p < 0.0005, **p < 0.005, *p < 0.05. E JMV7159 structure. F Western blot analysis of PXR, RXRalpha (RXRα), FXR, VDR, and GSPT1 protein expression in LS174T cells, treated 24 h with 0.1% DMSO or 5 µM JMV7048 or JMV7159. In cellulo detection of JMV compounds in live cells by fluorescence imaging (G) or flow cytometry analysis (H). Cells were treated with or without 5 μM JMV7048 or JMV7159 for 24 h.
