Mechanism of FACT removal from transcribed genes by anticancer drugs curaxins

Sci Adv. 2018 Nov 7;4(11):eaav2131. doi: 10.1126/sciadv.aav2131. eCollection 2018 Nov.

Abstract

Human FACT (facilitates chromatin transcription) is a multifunctional protein complex that has histone chaperone activity and facilitates nucleosome survival and transcription through chromatin. Anticancer drugs curaxins induce FACT trapping on chromatin of cancer cells (c-trapping), but the mechanism of c-trapping is not fully understood. Here, we show that in cancer cells, FACT is highly enriched within the bodies of actively transcribed genes. Curaxin-dependent c-trapping results in redistribution of FACT from the transcribed chromatin regions to other genomic loci. Using a combination of biochemical and biophysical approaches, we have demonstrated that FACT is bound to and unfolds nucleosomes in the presence of curaxins. This tight binding to the nucleosome results in inhibition of FACT-dependent transcription in vitro in the presence of both curaxins and competitor chromatin, suggesting a mechanism of FACT trapping on bulk nucleosomes (n-trapping).

Publication types

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

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Carbazoles / pharmacology*
  • Chromatin Assembly and Disassembly / drug effects
  • Chromatin Assembly and Disassembly / physiology*
  • Fibrosarcoma / drug therapy
  • Fibrosarcoma / genetics*
  • Fluorescence Resonance Energy Transfer
  • Histones / genetics
  • Histones / metabolism*
  • Humans
  • Nucleosomes / genetics
  • Nucleosomes / metabolism*
  • Promoter Regions, Genetic
  • Protein Binding
  • Transcription, Genetic / drug effects*
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • CBLC137
  • Carbazoles
  • Histones
  • Nucleosomes