| Literature DB >> 25219965 |
Junetha Syed1, Ganesh N Pandian2, Shinsuke Sato2, Junichi Taniguchi1, Anandhakumar Chandran1, Kaori Hashiya1, Toshikazu Bando1, Hiroshi Sugiyama3.
Abstract
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.Entities:
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Year: 2014 PMID： 25219965 DOI： 10.1016/j.chembiol.2014.07.019
Source DB: PubMed Journal: Chem Biol ISSN： 1074-5521