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).
- A8221 EPZ-64385 CitationSummary: EZH2 inhibitor, potent and selective
- B1583 UNC19992 CitationTarget: EZH2|EZH1Summary: EZH2 inhibitor
- B4989 EPZ015666Target: Protein Arginine MethyltransferasesSummary: PRMT5 inhibitor
- B6182 GSK591Target: PRMTSummary: PRMT5 inhibitor
- B1581 EPZ004777 HClTarget: DOT1LSummary: DOT1L inhibitor,potent and selective
- A8182 3-Deazaneplanocin A (DZNep) hydrochloride1 CitationTarget: EZH2Summary: SAHH and EZH2 inhibitor
- B7757 UNC 0642Target: G9a|GLPSummary: G9a and GLP histone lysine methyltransferase inhibitor
- A4166 EPZ56761 CitationTarget: DOT1LSummary: DOT1L inhibitor,potent and SAM competitive
- A4168 EntacaponeTarget: Catechol O-Methyltransferase (COMT)Summary: COMT inhibitor
- A4170 EPZ004777Target: DOT1LSummary: DOT1L inhibitor