Taking the Myc out of cancer: toward therapeutic strategies to directly inhibit c-Myc

Mol Cancer. 2021 Jan 4;20(1):3. doi: 10.1186/s12943-020-01291-6.


c-Myc is a transcription factor that is constitutively and aberrantly expressed in over 70% of human cancers. Its direct inhibition has been shown to trigger rapid tumor regression in mice with only mild and fully reversible side effects, suggesting this to be a viable therapeutic strategy. Here we reassess the challenges of directly targeting c-Myc, evaluate lessons learned from current inhibitors, and explore how future strategies such as miniaturisation of Omomyc and targeting E-box binding could facilitate translation of c-Myc inhibitors into the clinic.

Keywords: Leucine zipper; Oncogene; Peptide; Protein-protein interaction; Transcription.

Publication types

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

MeSH terms

  • Animals
  • Humans
  • Molecular Targeted Therapy
  • Neoplasms / drug therapy*
  • Peptides / pharmacology
  • Peptides / therapeutic use
  • Protein Binding
  • Proto-Oncogene Proteins c-myc / antagonists & inhibitors*
  • Proto-Oncogene Proteins c-myc / chemistry
  • Proto-Oncogene Proteins c-myc / metabolism
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology
  • Small Molecule Libraries / therapeutic use


  • Peptides
  • Proto-Oncogene Proteins c-myc
  • Small Molecule Libraries