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.
- B6784 NSC 95397Summary: Cdc25 dual specificity phosphatases inhibitor
- B6987 CI 976Summary: acyl-coenzyme A:cholesterol acyltransferase (ACAT) inhibitor
- B7241 VULM 1457Summary: Acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor
- B7250 YM 750Summary: Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor
- B7323 AGK 2Summary: SIRT2 inhibitor, potent and selective
- B7594 SalermideSummary: SIRT1 and SIRT2 inhibitor
- B7679 (R)-(+)-Etomoxir sodium saltSummary: carnitine palmitoyltransferase I (CPT1) inhibitor
- B7739 L002Summary: p300 inhibitor
- B7757 UNC 0642Target: G9a|GLPSummary: G9a and GLP histone lysine methyltransferase inhibitor
- B1127 UNC 0631Summary: G9a inhibitor