Histone Methyltransferase
Histone methyltransferases are a group of enzymes that catalyze the methylation of histone lysine and arginine by adding methyl groups to specific histone arginine or lysine residues. Histone methyltransferaes can be classified into 3 classes, including SET domain lysine methyltransferases, non-SET domain lysine methyltransferases and arginine methyltransferases (PRMTs), all of which use S-adenosylmethionine as a cosubstrate for the transfer of the methyl group. Aberrant histone methylation has been associated with a wide range of human cancers (such as hematological malignancies), which leads to the development of novel cancer chemotherapies targeting cancer-associated histone methyltransferases (more than 20 lysine methyltransferases and 9 arginine methyltransferases in humans).
- A4166 EPZ56761 CitationTarget: DOT1LSummary: DOT1L inhibitor,potent and SAM competitive
- A4168 EntacaponeTarget: Catechol O-Methyltransferase (COMT)Summary: COMT inhibitor
- A4171 EPZ0056872 CitationTarget: EZH2Summary: EZH2 inhibitor,potent and selective
- A4167 SGC 0946Summary: DOT1L inhibitor,highly potent and selective
- A4170 EPZ004777Target: DOT1LSummary: DOT1L inhibitor
- A1905 3-Deazaneplanocin,DZNep6 CitationTarget: HydrolaseSummary: S-adenosylhomocysteine and EZH2 inhibitor
- A1908 AMI-1Summary: PRMT1 inhibitor
- A1909 BIX 01294Target: G9aSummary: G9a and GLP inhibitor
- A1914 UNC06381 CitationSummary: G9a/GLP HMTase inhibitor, potent and selective
- A1146 Histone-H2A-(107-122)-Ac-OHSummary: Histone-H2A peptide