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. 2019 Nov 14;21(11):1110–1120. doi: 10.1016/j.neo.2019.10.003

Figure 3.

Figure 3

PROTACs dBET1 and MZ1 target BRD4 for degradation with repression of MYC expression and cell proliferation. (A) Western blot of BRD4 and MYC protein after incubation of LS174t cells with increased concentrations of dBET1 or MZ1 for 24 h. Shown are representative images of two independent experiments. (B) PROTAC-mediated BRD4 degradation correlates with reduction of MYC protein (r: Spearmańs rho coefficient). (C) PROTAC-mediated BRD4 degradation correlates with reduction of MYC mRNA. Shown are results as mean ± SD of three independent experiments. (D) Dose-response effects of dBET1 and MZ1 on LS174t cell growth assessed with crystal violet colony formation assay for a 3-day incubation. Shown are representative images of two independent experiments. (E) Western blot of BRD4 and MYC protein after incubation of fibroblasts with relevant concentrations of dBET1 or MZ1 for 24 h. Representative images of two independent experiments. (F) Western blot of BRD4 and MYC protein after incubation of “Patient Derived Organoid #T5” with relevant concentrations of dBET1 or MZ1 for 24 h.