2014年10月
Targeted Suppression of EVI1 Oncogene Expression by Sequence-Specific Pyrrole-Imidazole Polyamide
CHEMISTRY & BIOLOGY
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- 巻
- 21
- 号
- 10
- 開始ページ
- 1370
- 終了ページ
- 1380
- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.1016/j.chembiol.2014.07.019
- 出版者・発行元
- CELL PRESS
Human ectopic viral integration site 1 (EVI1) is an oncogenic transcription factor known to play a critical role in many aggressive forms of cancer. Its selective modulation is thought to alter the cancer-specific gene regulatory networks. Pyrrole-imidazole polyamides (PIPs) are a class of small DNA binders that can be designed to target any destined DNA sequence. Herein, we report a sequence-specific pyrrole-imidazole polyamide, PIP1, which can target specific base pairs of the REL/ELK1 binding site in the EVI1 minimal promoter. The designed PIP1 significantly inhibited EVI1 in MDA-MB-231 cells. Whole-transcriptome analysis confirmed that PIP1 affected a fraction of EVI1-mediated gene regulation. In vitro assays suggested that this polyamide can also effectively inhibit breast cancer cell migration. Taken together, these results suggest that EVI1-targeted PIP1 is an effective transcriptional regulator in cancer cells.
- リンク情報
- ID情報
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- DOI : 10.1016/j.chembiol.2014.07.019
- ISSN : 1074-5521
- eISSN : 1879-1301
- PubMed ID : 25219965
- Web of Science ID : WOS:000344521300016