Unknown,Transcriptomics,Genomics,Proteomics

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Antitumor activity of a pyrrole-imidazole polyamide


ABSTRACT: We report that a DNA minor groove binding hairpin pyrrole-imidazole (Py-Im) polyamide interferes with RNA polymerase II (RNAP2) activity in cell culture. Genome-wide mapping of RNAP2 binding shows reduction of occupancy preferentially at transcription start sites (TSS), while occupancy at enhancer sites are is unchanged. Genome-wide mapping of RNA polymerase II in LNCaP cells treated with DHT and DHT with Py-Im polyamide.

ORGANISM(S): Homo sapiens

SUBMITTER: Fei Yang 

PROVIDER: E-GEOD-43253 | biostudies-arrayexpress |

REPOSITORIES: biostudies-arrayexpress

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Publications

Antitumor activity of a pyrrole-imidazole polyamide.

Yang Fei F   Nickols Nicholas G NG   Li Benjamin C BC   Marinov Georgi K GK   Said Jonathan W JW   Dervan Peter B PB  

Proceedings of the National Academy of Sciences of the United States of America 20130114 5


Many cancer therapeutics target DNA and exert cytotoxicity through the induction of DNA damage and inhibition of transcription. We report that a DNA minor groove binding hairpin pyrrole-imidazole (Py-Im) polyamide interferes with RNA polymerase II (RNAP2) activity in cell culture. Polyamide treatment activates p53 signaling in LNCaP prostate cancer cells without detectable DNA damage. Genome-wide mapping of RNAP2 binding shows reduction of occupancy, preferentially at transcription start sites,  ...[more]

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