Nailing Down a Notoriously Elusive Cancer Target: Direct Inhibition of MYC by a Covalent Small Molecule.

Direct inhibition of the transcription factor MYC is widely recognized as one of the thorniest challenges in cancer drug discovery. In this issue of Cell Chemical Biology, Boike et al. (2020) discover a covalent MYC inhibitor that selectively targets a single cysteine residue in an unstructured region of the protein.