Figure 4.
Benzoselenoxanthene analogues down-regulate TMPRSS2 expression through stabilizing TMPRSS2 G-quadruplex. (A) Compounds down-regulated the transcription of TMPRSS2 mRNA. After Calu-3 cells were treated with compounds, TMPRSS2 mRNA was examined by qPCR after 24 h. (B) Compounds down-regulated the expression of TMPRSS2 protein (Uncropped images shown in Fig. S4). After Calu-3 cells were treated with compounds, TMPRSS2 protein was examined by western blot after 24 h. (C) Compounds repressed wild or mutant TMPRSS2 promoter activity through stabilizing TMPRSS2 G-quadruplex. A549 cells were transfected with wild (left) and G-rich section mutant (right) TMPRSS2 promoter vector, then treated with 2 μM of compounds, finally luciferase was detected in 24 h after treatment with compounds. All of experiments were repeated three times. Statistical significance was determined using Student’s two-tailed t-test (A,C). *P < 0.05, **P < 0.01, ***P < 0.001. Error bars represent the SEM of three independent experiments.