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


  • eng