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

Matthew J Henley; Shelby K Doyle; Angela N Koehler

doi:10.1016/j.chembiol.2020.12.014

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

Cell Chem Biol. 2021 Jan 21;28(1):1-3. doi: 10.1016/j.chembiol.2020.12.014.

Authors

Matthew J Henley¹, Shelby K Doyle¹, Angela N Koehler²

Affiliations

¹ David H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02142, USA.
² David H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02142, USA. Electronic address: koehler@mit.edu.

PMID: 33482085
DOI: 10.1016/j.chembiol.2020.12.014

Abstract

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.

Publication types

Comment

MeSH terms

Antineoplastic Agents* / pharmacology
Cysteine
Drug Discovery
Fracture Fixation, Intramedullary*
Neoplasms* / drug therapy
Transcription Factors

Substances

Antineoplastic Agents
Transcription Factors
Cysteine