Chromatin/Epigenetics
Epigenetics is the heritable modifications in gene expression that is not associated with changes in DNA sequence. Epigenetic modifications occur mostly on DNA or on the histone octamer. There are several types of epigenetics modifications, DNA methylation by DNA-methyl transferase (DNMT) and covalent modification of histones (e.g. acetylation, methylation, phosphorylation and ubiquitination). Histone acetylation by histone acetyltransferases (HATs) is involved in transcriptional activation, whereas histone deacetylation by histone deacetylases (HDACs) is connected with transcriptional repression. Histone demethylation is associated with lysine-specific demethylase (LSD) and JmjC domain containing histone demethylase (JHDM).
The nucleosome is consisted of four histone proteins (H2A, H2B, H3, and H4), they are primary building block of chromatin. The addition and removal of specific chemical groups refers to as epigenetic marks, it regulates chromatin structure and affects gene expression. Moreover, RNA is intimately involved in the formation of a repressive chromatin state.
Epigenetic mechanism responds to environmental changes at the cellular level and thus influences cellular plasticity. Chromatin and epigenetic regulation play a significant role in the programming of the genome during development and stress response, defects in epigenetics can lead to cancer, inflammation and metabolic disorders etc.
- B3272 InauhzinTarget: Sir2-like Family Deacetylases (Sirtuins)Summary: SIRT1 inhibitor
- A3012 Ruxolitinib (INCB018424)4 CitationTarget: JAKSummary: JAK inhibitor
- A4083 Rocilinostat (ACY-1215)1 CitationTarget: Histone Deacetylases (HDACs)Summary: Selective HDAC6 inhibitor
- A4084 Vorinostat (SAHA, MK0683)9 CitationTarget: Histone Deacetylases (HDACs)Summary: HDAC inhibitor
- A4089 Mocetinostat (MGCD0103, MG0103)2 CitationTarget: Histone Deacetylases (HDACs)Summary: HDAC inhibitor,isotype-selective and potent
- A4090 JNJ-264815853 CitationTarget: Histone Deacetylases (HDACs)Summary: Potent HDAC inhibitor
- A4092 CUDC-1011 CitationTarget: Histone Deacetylases (HDACs)|EGFR|ErbBSummary: Multitargeted HDAC inhibitor
- A4137 AZD1480Target: JAKSummary: JAK2 inhibitor,ATP-competitive and novel
- A4140 WP1066Target: STAT|JAKSummary: JAK2/STAT3 inhibitor,cell-permeable
- A4147 LY2784544Target: Aurora Kinases|FLT3|VEGFR|FGFR|Trk Receptors|JAK|ALK|TYK2|MUSK|MAP3KSummary: JAK2 inhibitor,highly potent and selective