Synthetic ligand promotes gene expression by affecting GC sequence in promoter

Bioorg Med Chem Lett. 2017 Aug 1;27(15):3391-3394. doi: 10.1016/j.bmcl.2017.06.006. Epub 2017 Jun 3.

Abstract

A naphthyridine carbamate tetramer (NCT8) is a synthetic compound, which selectively binds to nucleic acids containing CGG/CGG sequence. Although NCT8 is a promising compound for a wide range of DNA and RNA based biotechnology such as modulation of specific gene expression, little is known about its behavior in human cells. In the present study, we investigated the changes induced in gene expression by NCT8. Genes differentially expressed in the presence of NCT8 in HeLa cells were identified by whole-transcriptome analysis. The whole-transcriptome analysis showed that NCT8 significantly induced up-regulation of specific genes, whose promoter region has GC-rich sequence.

Keywords: Mismatch binding ligand; RNA-Seq; Regulation of gene expression.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Carbamates / chemical synthesis
  • Carbamates / chemistry
  • Carbamates / pharmacology*
  • Dose-Response Relationship, Drug
  • GC Rich Sequence / genetics*
  • HeLa Cells
  • Humans
  • Ligands
  • Molecular Structure
  • Naphthyridines / chemical synthesis
  • Naphthyridines / chemistry
  • Naphthyridines / pharmacology*
  • Promoter Regions, Genetic / drug effects*
  • Promoter Regions, Genetic / genetics*
  • Structure-Activity Relationship
  • Up-Regulation / drug effects*

Substances

  • Carbamates
  • Ligands
  • Naphthyridines