Myc proto-oncogene protein (c-Myc) (c-Myc)

Myc proto-oncogene protein (c-Myc) is a master transcription factor that regulates the expression of approximately 15% of all human genes, primarily those involved in cell growth, proliferation, and metabolism (UniProt P01106). It functions by forming a heterodimer with its partner protein, MAX, which then binds to E-box sequences in the promoter regions of target genes (PubMed: 29123071). In healthy cells, c-Myc expression is tightly controlled; however, in over 70% of human cancers, it is constitutively expressed or amplified, driving uncontrolled cell division and metabolic reprogramming (PubMed: 32958953). Historically, c-Myc was considered "undruggable" due to its lack of a deep binding pocket and its intrinsically disordered structure (PubMed: 34108471). Current therapeutic strategies focus on disrupting the MYC-MAX interaction, inhibiting MYC transcription via BET inhibitors like OTX015, or utilizing mini-proteins like Omomyc to sequester MYC from DNA (PubMed: 31036548). Despite its potential as a "silver bullet" for cancer, targeting c-Myc poses significant safety challenges because of its essential role in the maintenance of normal stem cell populations and regenerative tissues (PubMed: 28335025).

Other names

MYCbHLHe39Proto-oncogene c-MycTranscription factor p64Class E basic helix-loop-helix protein 39Avian myelocytomatosis virus oncogene homolog

Inhibition of MYC-MAX heterodimerization, disruption of MYC-DNA binding, transcriptional downregulation through BET bromodomain inhibition, and induction of MYC protein degradation (PubMed: 34108471, PubMed: 31036548).