Taking the Myc out of Cancer: Toward Therapeutic Strategies to Directly Inhibit c-Myc

Sarah Madden, Aline Dantas de Araujo, Mara Gerhardt, David Fairlie, Jody Mason

Research output: Contribution to journalReview articlepeer-review

178 Citations (SciVal)

Abstract

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.
Original languageEnglish
Article number3
JournalMolecular Cancer
Volume20
Issue number1
DOIs
Publication statusPublished - 4 Jan 2021

Bibliographical note

Funding Information:
JMM is grateful to Cancer Research UK (A26941). JMM and DPF also wish to thank the Medical Research Council (MRC) (MR/T028254/1) and the Biotechnology and Biological Sciences Research Council (BBSRC) (BB/R017956/1, BB/T018275/1). DPF thanks the National Health and Medical Research Council of Australia (NHMRC) for a Senior Principal Research Fellowship (1117017) and the Australian Research Council for grant support (CE140100011).

Publisher Copyright:
© 2021, The Author(s).

Keywords

  • Leucine zipper
  • Oncogene
  • Peptide
  • Protein-protein interaction
  • Transcription

ASJC Scopus subject areas

  • Molecular Medicine
  • Oncology
  • Cancer Research

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