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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).

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  2. A4171 EPZ005687 EZH2 inhibitor,potent and selective
  3. B4989 EPZ015666 PRMT5 inhibitor
  4. B6088 EPZ020411 PRMT6 inhibitor
  5. B6082 EPZ031686 SMYD3 inhibitor
  6. A4166 EPZ5676 DOT1L inhibitor,potent and SAM competitive
  7. B6182 GSK591 PRMT5 inhibitor
  8. A1146 Histone-H2A-(107-122)-Ac-OH Histone-H2A peptide
  9. B7806 HLCL-61 PRMT5 inhibitor
  10. B6119 LLY507 SMYD2 inhibitor
  11. B1582 MM-102 MLL1 inhibitor,high-affinity peptidomimetic

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