This article published in Nature describes a first-in-class METTL3 inhibitor for the treatment of acute Myeloid Leukaemia.
The publication covers:
- Development of STM2457 following high-throughput screen
- Selectivity screening across the panel of 45 human methyltransferases
- Crystal structure of METTL3-14 complex with STM2457, part of structure-based drug design strategy for this target
- Compound validation in cellular assays and in vivo efficacy