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.
- B1583 UNC19992 CitationTarget: EZH2|EZH1Summary: EZH2 inhibitor
- B1251 Valproic acidTarget: Histone Deacetylases (HDACs)Summary: HDAC1 inhibitor
- B1498 I-BET-7624 CitationTarget: BromodomainsSummary: BET inhibitor,highly potent
- B1500 I-BET151 (GSK1210151A)2 CitationTarget: Bromodomain and Extra-Terminal motif (BET)Summary: Selective BET inhibitor
- B8023 Cerdulatinib (PRT062070)Target: JAK|Syk|TYK2Summary: Syk/JAK inhibitor
- B4875 PFI-21 CitationTarget: SETD7Summary: SETD7 methyltransferase inhibitor
- B4887 RemodelinTarget: NAT10Summary: NAT10 inhibitor
- B4890 HPOB1 CitationTarget: Histone Deacetylases (HDACs)Summary: HDAC6 inhibitor, potent and selective
- B4894 SP2509Target: Histone DemethylasesSummary: Demethylase 1 (LSD1) antagonist, novel Lysine-specific
- A8708 Sephin11 CitationTarget: phosphatasesSummary: Selective PPP1R15A inhibitor