Fig. 4: Simple and rapid screening of various PROTACs achieved by ESR in vitro. | Nature Communications

Fig. 4: Simple and rapid screening of various PROTACs achieved by ESR in vitro.

From: Non-invasive in vivo monitoring of PROTAC-mediated protein degradation using an environment-sensitive reporter

Fig. 4

a Chemical structures of BRD4-PROTACs. b The characterization of BRD4-PROTACs. The terms C and O refer to the number of carbon and oxygen atoms in the linker. c Schematic illustration of JQ1-NR for screening BRD4-PROTACs. d Flow cytometry analysis of the JQ1-NR fluorescent signals in cells incubated with various BRD4-PROTACs. (Data are presented as mean value ± SD, experiments were repeated three times) (e) Heat map shows the heterogeneity of efficacy of the same protein degrader in various cell lines. f Fluorescence imaging of the JQ1-NR (2 μM, 1 h) in different cell lines pretreated with various BRD4-PROTACs (100 nM) using an IVIS spectrum imaging system (Ex/Em = 500/620 nm). (g) Western blotting analysis of BRD4 levels in 4T1 cells treated with different BRD4-PROTACs (100 nM) (n = 3 independent experiments). h Quantification of (g) (Data are presented as mean value ± SD, n = 3 independent experiments). i Correlation between the JQ1-NR signals (4T1 cells) in (d) and relative BRD4 expression measured in (h). Pearson r and P values were derived using a simple linear regression model, two-tailed Student t-test analysis. Source data are provided as a Source Data file.

Back to article page