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Fig. 5 | Cell & Bioscience

Fig. 5

From: BRD4 inhibitor GNE987 exerts anti-cancer effects by targeting super-enhancers in neuroblastoma

Fig. 5

GNE987 is a BET-targeting PROTAC based on VHL, for which the BET protein degradation is proteasome-dependent. A Bifunctional PROTAC molecules bind to the targeting-protein (BRD4, dark green) with one end (a motif, light green) while the other end (a motif, light blue) binds to an E3-ubiquitin ligase (dark blue) to form a ternary complex. The recruited E3 ligase then mediates the transfer of ubiquitin from an E2 enzyme to the targeted protein (direction of arrow). B Analysis of VHL expression in the IMR-32 and SK-N-BE (2) cells treated with negative control sh-NC (or PLVX-NC) and sh-VHL (or PLVX-VHL) examined by Western blotting. Then the sensitivity to GNE987 of the NB cells transfected with sh-VHL (or PLVX-VHL) and NB cells transfected with sh-NC (or PLVX-NC) was compared. *p < 0.05, **p < 0.01, ***p < 0.001, ****p < 0.0001. C Western blotting analysis of the BET protein in SK-N-BE (2) and IMR-32 cells treated with the 5 nM GNE987 and series concentrations of MG132, and their combination for 24 h

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