title: Hijacked in cancer: the KMT2 (MLL) family of methyltransferases.
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.
authors.affiliation: 1] Department of Pathology, University of Michigan. [2] Department of Ophthalmology &Visual Sciences, University of Michigan.
authors.forename: Rajesh C
authors.initials: RC
authors.lastname: Rao
authors.affiliation: 1] Department of Pathology, University of Michigan. [2] Department of Biological Chemistry, University of Michigan, Ann Arbor, Michigan 48109, USA.
authors.forename: Yali
authors.initials: Y
authors.lastname: Dou
mesh_terms: D011495:Histone-Lysine N-Methyltransferase / Q000737:chemistry* / Q000235:genetics / Q000378:metabolism*; D006801:Humans; D058990:Molecular Targeted Therapy; D009154:Mutation; D051788:Myeloid-Lymphoid Leukemia Protein / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D009369:Neoplasms / Q000201:enzymology* / Q000235:genetics* / Q000378:metabolism; D021122:Protein Subunits
chemical_list: C497422:KMT2A protein, human; D021122:Protein Subunits; D051788:Myeloid-Lymphoid Leukemia Protein; D011495:Histone-Lysine N-Methyltransferase