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Cancer Sci. 2014 Oct;105(10):1272-8. doi: 10.1111/cas.12493. Epub 2014 Sep 18.

Pyrrole-imidazole polyamide targeted to break fusion sites in TMPRSS2 and ERG gene fusion represses prostate tumor growth.

Author information

1
Department of Urology, Nihon University School of Medicine, Tokyo, Japan; Department of Anti-Aging Medicine, Graduate School of Medicine, The University of Tokyo, Tokyo, Japan.

Abstract

Aberrant overexpression of ERG induced by the TMPRSS2-ERG gene fusion is likely involved in the development of prostate cancer. Synthetic pyrrole-imidazole (PI) polyamides recognize and attach to the minor groove of DNA with high affinity and specificity. In the present study, we designed a PI polyamide targeting TMPRSS2-ERG translocation breakpoints and assessed its effect on human prostate cancer cells. Our study identified that this PI polyamide repressed the cell and tumor growth of androgen-sensitive LNCaP prostate cancer cells. Targeting of these breakpoint sequences by PI polyamides could be a novel approach for the treatment of prostate cancer.

KEYWORDS:

Androgen receptor; TMPRSS2-ERG; fusion gene; prostate cancer; pyrrole-imidazole polyamide

PMID:
25088707
PMCID:
PMC4462350
DOI:
10.1111/cas.12493
[Indexed for MEDLINE]
Free PMC Article

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