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. 2022 Sep 28;23(1):1–15. doi: 10.1080/15384047.2022.2125748

Figure 5.

Figure 5.

VHL is a powerful helper for MZ1 in AML cell lines; BRD4 protein degradation is dependent on the ubiquitin-proteasome system. (a) Western blot analysis of VHL protein expression in AML cell lines. (b) Schematic illustration of the bifunctional PROTAC molecule (MZ1). (c) sh-VHL or PLVX-VHL lentivirus was transfected into NB4 and Kasumi-1 cells, and the expression level of VHL was detected by Western blot. (d) Comparison of the sensitivity of VHL knockdown or overexpressed NB4 and Kasumi-1 cells. VHL downregulation increased the IC50 of MZ1 in NB4 and Kasumi-1 cells; VHL overexpression decreased the IC50 of MZ1 in NB4 and Kasumi-1 cells. (e) After MZ1 treatment (0.25μΜ) of Kasumi-1 and K562 cells and different concentrations of MG132 for 12 h, Western blot showed that MG132 inhibited BRD2, BRD3 and BRD4 protein degradation in a dose-dependent manner. Each concentration was tested in triplicate and independently performed at least three times. *p < .05, **p < .01, ***p < .001, ****p < .0001.