초록 |
Epigenetic alterations have been involved in the pathogenesis of cancer and auto-immune diseases, including Crohn’s Disease, Ulcerative Colitis, Lupus and Rheumatoid Arthritis. Histone deacetylases (HDACs), a key component of the epigenetic machinery, are enzymes that catalyze the removal of acetyl functional groups from the lysine residues of both histone and non-histone proteins. There are 18 isotypes of HDACs with different functions in different disease settings. Therefore, the development of HDAC inhibitor with isoform-selectivity may provide important new tools for treatment of auto-immune diseases. To date, MC-1568 (MJK001) analogues were designed and synthesized to target HDAC9 for treatment of inflammatory bowel disease (IBD), one of the auto-immune diseases. |