G4 DNA in ras genes and its potential in cancer therapy

Biochim Biophys Acta. 2016 Apr;1859(4):663-74. doi: 10.1016/j.bbagrm.2016.02.002. Epub 2016 Feb 4.

Abstract

It is now well established that in the human genome the canonical double helix coexists with folded G-quadruplex structures that are known to have important biological functions. In this review we summarize the current knowledge on quadruplex formation in the promoters of the ras genes that are mutated in about 30% of all human cancers. We describe the nuclear proteins that recognize these unusual DNA structures and discuss their function in transcription. We also examine the formation of G-quadruplexes in the 5'-untranslated region of the ras transcripts and conclude this review by reporting strategies that use either ras G-quadruplexes or proteins recognizing the ras G-quadruplexes as targets of anticancer small molecules.

Keywords: 5′-UTR; Antigene strategies; G-quadruplex; HRAS; KRAS; NRAS; Promoter.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • 5' Untranslated Regions / genetics
  • G-Quadruplexes*
  • Genome, Human
  • Humans
  • Neoplasms / genetics*
  • Neoplasms / therapy
  • Promoter Regions, Genetic
  • Proto-Oncogene Proteins p21(ras) / genetics*
  • Small Molecule Libraries / therapeutic use
  • Transcription, Genetic*

Substances

  • 5' Untranslated Regions
  • Small Molecule Libraries
  • HRAS protein, human
  • Proto-Oncogene Proteins p21(ras)