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

Molecular Cancer

Sarah K. Madden¹  Mara Gerhardt¹  Jody M. Mason¹  Aline Dantas de Araujo²  David P. Fairlie² 

[1]Department of Biology & Biochemistry, University of Bath

[2]Division of Chemistry and Structural Biology and ARC 1066 Centre of Excellence for Innovations in Peptide and Protein Science, Institute for Molecular Bioscience, The University of Queensland

关键词: Oncogene;    Transcription;    Leucine zipper;    Peptide;    Protein-protein interaction;   

DOI  :  10.1186/s12943-020-01291-6

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown