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. Author manuscript; available in PMC: 2021 Apr 15.
Published in final edited form as: J Am Chem Soc. 2020 Apr 1;142(15):6970–6982. doi: 10.1021/jacs.9b13159

Figure 8.

Figure 8.

Bioactivity of the dimer-bleomycin conjugate 5 in DU-145 prostate cancer cells. (A) Effect of cleaving compound 5 and negative control compound 6 on pri-miR-17–92 levels in DU-145 cells, as determined by RT-qPCR. (B) Competition experiment between dimer binder 2 and 5 and their effect of pri-miR-17–92 levels, as determined by RT-qPCR. (C) Effect of 5 on pre-miR-17 levels, as determined by RT-qPCR. (D) Effect of 5 on the levels of mature miRNAs derived from the miR-17–92 cluster, as determined by RT-qPCR. (E) Effect of 5 on Stk4 mRNA levels, a direct target of miR-18a, as determined by RT-qPCR. (F) Effect of 5 on Caspase 3/7 activity, an indicator of apoptosis which is impeded in DU-145 cells due to repression of STK4. (G) Profiling of 373 miRNAs in DU-145 cells shows that only mature miRNAs derived from the 17–92 cluster are significantly affected, with miR-17 and −18a being the most significantly affected. Note that profiling was completed after a 6 h treatment period to minimize downstream effects as the compound induces apoptosis. All other data were collected after at 24 h treatment period. Errors are reported as SEM *, p < 0.05; **, p < 0.01; ***, p < 0.001, as determined by a Student t test.