First-in-class inhibitors of the protein lysine methyltransferase METTL21A

This is the authors' abstract. We don't add key points for this paper.

1.10 μM. We solved a crystal structure of METTL21A in complex with 6m (HK474), providing structural insight into ligand recognition and supporting further structure-guided optimization. These findings establish a biochemically and structurally validated starting point for probing METTL21A function and a foundation for the development of cellularly active METTL21A-targeted chemical tools.