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. 2015 Jun 2;10(8):1770–1777. doi: 10.1021/acschembio.5b00216

Figure 4.

Figure 4

Selective degradation of BRD4 leads to a differential response between JQ1 and MZ1 on selected genes. mRNA expression profiles of MYC, P21, AREG, FAS, FGFR1, and TYRO3 upon treatment with PROTAC MZ1 and JQ1 were compared. (a) HeLa cells were treated with 100 nM MZ1, VHL-1′, or JQ1 or 0.01% DMSO vehicle control (Veh.) for 24 h. (b) To mimic the protein removal effect, HeLa cells were transfected with siRNA targeting individual BRD2, BRD3, or BRD4 or negative control siRNA and were harvested after 48 h. Quantitative PCR was performed to analyze relative gene expression level of treated HeLa cells using target specific primers. Gene expression levels relative to GAPDH were normalized to control treatment. The data shown represent the mean ± SEM (n = 3 technical replicates) of one experiment. Statistical significance compared to the control was determined with two-tailed t tests: *P < 0.05, **P < 0.01, ***P < 0.001, and n.s. = not significant.