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.
- A8221 EPZ-64385 CitationSummary: EZH2 inhibitor, potent and selective
- A1877 XAV-9391 CitationTarget: TNKSSummary: Tankyrase 1/2 inhibitor
- A8302 Tenovin-6Target: Sir2-like Family Deacetylases (Sirtuins)Summary: SIRT inhibitor and p53 activator
- A8547 Tubastatin A HCl1 CitationTarget: Histone Deacetylases (HDACs)Summary: HDAC6 inhibitor,potent and selective
- A8803 RGFP9664 CitationTarget: Histone Deacetylases (HDACs)Summary: Specific HDAC3 inhibitor
- A8807 MK-8745Target: Aurora KinasesSummary: Aurora A inhibitor,potent and selective
- B1500 I-BET151 (GSK1210151A)2 CitationTarget: Bromodomain and Extra-Terminal motif (BET)Summary: Selective BET inhibitor
- B4890 HPOB1 CitationTarget: Histone Deacetylases (HDACs)Summary: HDAC6 inhibitor, potent and selective
- B4894 SP2509Target: Histone DemethylasesSummary: Demethylase 1 (LSD1) antagonist, novel Lysine-specific
- B4989 EPZ015666Target: Protein Arginine MethyltransferasesSummary: PRMT5 inhibitor