Science Pool

Small-Molecule Inhibition of METTL3 as a Strategy Against Myeloid Leukaemia

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