A Synthetic Transcriptional Activator of Genes Associated with the Retina in Human Dermal Fibroblasts

Chembiochem. 2015 Jul 6;16(10):1497-501. doi: 10.1002/cbic.201500140. Epub 2015 May 28.

Abstract

Small molecules capable of modulating epigenetic signatures can activate the transcription of tissue-restricted genes in a totally unrelated cell type and have potential use in epigenetic therapy. To provide an example for an initial approach, we report here on one synthetic small-molecule compound-termed "SAHA-PIP X"-from our library of conjugates. This compound triggered histone acetylation accompanied by the transcription of retinal-tissue-related genes in human dermal fibroblasts (HDFs).

Keywords: DNA recognition; artificial transcription activators; gene expression; histone acetylation; transcription profiling.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylation / drug effects*
  • Cell Line
  • Epigenesis, Genetic / drug effects
  • Fibroblasts / drug effects*
  • Fibroblasts / metabolism
  • Gene Expression Profiling
  • Histones / genetics
  • Histones / metabolism*
  • Humans
  • Imidazoles / chemistry
  • Imidazoles / pharmacology
  • Pyrroles / chemistry
  • Pyrroles / pharmacology*
  • Retina / metabolism*
  • Retinal Diseases / genetics
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology*
  • Transcriptional Activation / drug effects*

Substances

  • Histones
  • Imidazoles
  • Pyrroles
  • Small Molecule Libraries