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. 2019 Sep 17;5(10):1682–1690. doi: 10.1021/acscentsci.9b00713

Figure 4.

Figure 4

PhotoPROTAC-1 can be converted to active trans- and inactive cis-isomers to induce differential degradation of BRD2. PhotoPROTAC-1 working solutions were irradiated for 30 min using 415 or 530 nm LEDs and added to Ramos cells at varying concentrations. Cells were incubated in the dark for (A) 6.5 h or (B) 18 h prior to cell lysis. Treatment of active trans-photoPROTAC induced significant BRD2 degradation within 6.5 h whereas inactive cis-photoPROTAC-1 did not show a significant effect on BRD2 levels. BRD4 degradation was not observed under indicated conditions. (C) Time-dependent degradation of BRD proteins by photoPROTAC-1. Singly irradiated photoPROTAC-1 (trans and cis) were treated at 500 nM concentrations, and BRD protein levels were analyzed after indicated time points.