Targeting MYC by disrupting interaction with WDR5 

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Crystal structure of WDR5 in complex with a MbIIIb peptide. This structure was solved by our collaborator, Dr. Stephen Fesik, and co-workers. WDR5 is a seven-bladed β-propellor structure; the MbIIIb peptide is shown in blue. MbIIIb engages a shallow, hydrophobic, cleft on one surface of WDR5. Genetic evidence shows this interaction is critical for MYC-driven tumors. Can it be targeted by drug-like molecules to perturb MYC activity in cancer?

© Bill Tansey 2021