Identification of novel inhibitors that disrupt STAT3-DNA interaction from a γ-AApeptide OBOC combinatorial library

Chem Commun (Camb). 2014 Aug 14;50(63):8739-42. doi: 10.1039/c4cc03909b. Epub 2014 Jun 25.

Abstract

From a γ-AApeptide-based one-bead-one-compound (OBOC) combinatorial library, we identified γ-AApeptides that can selectively inhibit STAT3-DNA interaction and suppress the expression levels of STAT3 target genes in intact cells. Our results demonstrate that in addition to the SH2 domain, the DNA binding domain of STAT3 is targetable for the development of a new generation of anti-cancer therapeutics.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Combinatorial Chemistry Techniques
  • DNA / drug effects*
  • Female
  • Humans
  • Models, Molecular
  • Molecular Conformation
  • Peptide Library
  • Peptides / chemical synthesis*
  • Peptides / chemistry
  • Peptidomimetics / chemical synthesis*
  • Peptidomimetics / pharmacology*
  • STAT3 Transcription Factor / drug effects*
  • src Homology Domains / drug effects

Substances

  • Antineoplastic Agents
  • Peptide Library
  • Peptides
  • Peptidomimetics
  • STAT3 Transcription Factor
  • DNA