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

Figure 5.

Figure 5

PhotoPROTACs are dynamically interchangeable between active trans- and inactive cis-configurations. (A) PhotoPROTAC-1 working solutions were initially irradiated with 415 or 530 nm LEDs followed by second irradiation using 530 or 415 nm (415/530 and 530/415 nm) to reverse the initial configurations. The treatment of singly irradiated trans-photoPROTAC-1 (415 nm) induced a significant BRD2 degradation relative to the cis-photoPROTAC-1 (530 nm) whereas no significant BRD4 degradation was observed in response to both trans- and cis-photoPROTAC-1. Second irradiation with either 530 or 415 nm significantly shifted the biologically active trans-isomer to inactive cis-isomer and vice versa. (B) Temporal control of photoPROTAC-1 activity. Singly irradiated photoPROTAC-1 (trans/415 nm and cis/530 nm) were added to cells. One set of cis- and trans-photoPROTAC-1 treated cells were kept in the dark, and a parallel set of cells treated with trans-photoPROTAC-1 were exposed to irradiation at 530 nm (415 initial/530 nm in cells) to induce the trans to cis isomerization in cells.