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Nat Rev Cancer. 2015 Jun;15(6):334-46. doi: 10.1038/nrc3929.

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

Author information

1
1] Department of Pathology, University of Michigan. [2] Department of Ophthalmology &Visual Sciences, University of Michigan.
2
1] Department of Pathology, University of Michigan. [2] Department of Biological Chemistry, University of Michigan, Ann Arbor, Michigan 48109, USA.

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.

PMID:
25998713
PMCID:
PMC4493861
DOI:
10.1038/nrc3929
[Indexed for MEDLINE]
Free PMC Article
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