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.
- B4946 GarcinolSummary: Inhibitor of PCAF and p300 histone acetyltransferase (HAT) activity
- B4947 A 366Summary: G9a/GLP histone lysine methyltransferase inhibitor
- B4948 UNC 2400Summary: negative control of UNC1999
- B4949 WDR5 0103Summary: WD repeat-containing protein 5 (WDR5) antagonist
- A8708 Sephin11 CitationTarget: phosphatasesSummary: Selective PPP1R15A inhibitor
- B4983 GSK-LSD1 2HClSummary: irreversible, and selective LSD1 inhibitor
- B4989 EPZ015666Target: Protein Arginine MethyltransferasesSummary: PRMT5 inhibitor
- A8712 MCB-613Target: SrcSummary: stimulator of steroid receptor coactivator (SRC)
- B5959 GSK J4 free baseSummary: histone demethylase JMJD3/UTX inhibitor
- B5861 Molidustat (BAY85-3934)Target: HIF-PHSummary: Novel HIF-PH inhibitor