Journal
CANCER SCIENCE
Volume 105, Issue 10, Pages 1272-1278Publisher
WILEY
DOI: 10.1111/cas.12493
Keywords
Androgen receptor; fusion gene; prostate cancer; pyrrole-imidazole polyamide; TMPRSS2-ERG
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Funding
- Ministry of Education, Culture, Sports, Science and Technology (MEXT), Japan
- Strategic Research Foundation for Private Universities from the MEXT
- Japan Society for the Promotion of Science, Japan
- Nihon University Medical Alumni Association
- Japanese Urological Association
- Program for Promotion of Fundamental Studies in Health Sciences, National Institute of Biomedical Innovation, Japan
- Grants-in-Aid for Scientific Research [25293214, 23249040, 26861302, 25871150, 221S0001, 25670678] Funding Source: KAKEN
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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.
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