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.
- B1499 RVX-2082 CitationSummary: Potent BET bromodomain inhibitor
- B1582 MM-1021 CitationSummary: MLL1 inhibitor,high-affinity peptidomimetic
- B1583 UNC19992 CitationTarget: EZH2|EZH1Summary: EZH2 inhibitor
- B1622 SGI-1027Summary: DNMT inhibitor
- B1141 Varenicline HydrochlorideSummary: α4β2 nicotinic receptor agonist
- B1251 Valproic acidTarget: Histone Deacetylases (HDACs)Summary: HDAC1 inhibitor
- B1163 MK-4827 hydrochlorideSummary: PARP1/PARP2 inhibitor
- B1164 MK-4827 tosylateSummary: PARP1/PARP2 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