Gene expression changes in a tumor xenograft by a pyrrole-imidazole polyamide.
Journal Article (Journal Article)
Gene regulation by DNA binding small molecules could have important therapeutic applications. This study reports the investigation of a DNA-binding pyrrole-imidazole polyamide targeted to bind the DNA sequence 5'-WGGWWW-3' with reference to its potency in a subcutaneous xenograft tumor model. The molecule is capable of trafficking to the tumor site following subcutaneous injection and modulates transcription of select genes in vivo. An FITC-labeled analogue of this polyamide can be detected in tumor-derived cells by confocal microscopy. RNA deep sequencing (RNA-seq) of tumor tissue allowed the identification of further affected genes, a representative panel of which was interrogated by quantitative reverse transcription-PCR and correlated with cell culture expression levels.
Full Text
Duke Authors
Cited Authors
- Raskatov, JA; Nickols, NG; Hargrove, AE; Marinov, GK; Wold, B; Dervan, PB
Published Date
- October 2012
Published In
Volume / Issue
- 109 / 40
Start / End Page
- 16041 - 16045
PubMed ID
- 22988074
Pubmed Central ID
- PMC3479560
Electronic International Standard Serial Number (EISSN)
- 1091-6490
International Standard Serial Number (ISSN)
- 0027-8424
Digital Object Identifier (DOI)
- 10.1073/pnas.1214267109
Language
- eng