Efficacy of novel pyrrole-imidazole (PI) polyamides targeting of TMPRSS2-ERG gene fusion for prostate cancer cells

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We developed a novel compounds, which controls a prostate specific fusion gene TMPSS2-ERG. By using Synthetic pyrrole-imidazole (PI) polyamides, that recognize and attach to the minor groove of DNA with high affinity and specificity, we examined the effects of a TMPRSS2-ERG translocation breakpoints-targeted PI polyamide on prostate cancer. Human prostate cancer cell line LNCaP which has TMPRSS2-ERG by DHT stimulation or genotoxic stress was used for analysis. Treatment of this polyamide showed the repression of chromosomal translocation and TMPRSS2-ERG expression in LNCaP. In addition, this polyamide decreased cell growth rate and cell migration.Moreover, we designed polyamides targeting for androgen receptor coregulator binding motif.