Hijacked in cancer: the KMT2 (MLL) family of methyltransferases

RC Rao, Y Dou - Nature Reviews Cancer, 2015 - nature.com
Nature Reviews Cancer, 2015nature.com
Abstract Histone–lysine N-methyltransferase 2 (KMT2) family proteins methylate lysine 4 on
the histone H3 tail at important regulatory regions in the genome and thereby impart crucial
functions through modulating chromatin structures and DNA accessibility. Although the
human KMT2 family was initially named the mixed-lineage leukaemia (MLL) family, owing to
the role of the first-found member KMT2A in this disease, recent exome-sequencing studies
revealed KMT2 genes to be among the most frequently mutated genes in many types of …
Abstract
Histone–lysine N-methyltransferase 2 (KMT2) family proteins methylate lysine 4 on the histone H3 tail at important regulatory regions in the genome and thereby impart crucial functions through modulating chromatin structures and DNA accessibility. Although the human KMT2 family was initially named the mixed-lineage leukaemia (MLL) family, owing to the role of the first-found member KMT2A in this disease, recent exome-sequencing studies revealed KMT2 genes to be among the most frequently mutated genes in many types of human cancers. Efforts to integrate the molecular mechanisms of KMT2 with its roles in tumorigenesis have led to the development of first-generation inhibitors of KMT2 function, which could become novel cancer therapies.
nature.com