Targeting menin.

摘要

The mixed lineage leukaemia (MLL) gene, which encodes a histone methyltransferase, is frequently translocated in human acute leukaemias. The interaction of MLL with menin is known to be essential for the oncogenic activity of MLL-fusion proteins; therefore, targeting this interaction could have therapeutic relevance. Jolanta Grembecka, Tomasz Cierpicki and colleagues have previously characterized the interaction between MLL and menin, which requires the amino terminus of MLL, and this part of the protein remains intact in all MLL-fusion proteins studied to date. The authors used high-throughput screening to identify compounds that target menin and that suppress its interaction with MLL.