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
- B1583 UNC19992 CitationTarget: EZH2|EZH1Summary: EZH2 inhibitor
- B4989 EPZ015666Target: Protein Arginine MethyltransferasesSummary: PRMT5 inhibitor
- B6182 GSK591Target: PRMTSummary: PRMT5 inhibitor
- B1581 EPZ004777 HClTarget: DOT1LSummary: DOT1L inhibitor,potent and selective
- A8182 3-Deazaneplanocin A (DZNep) hydrochloride1 CitationTarget: EZH2Summary: SAHH and EZH2 inhibitor
- B7757 UNC 0642Target: G9a|GLPSummary: G9a and GLP histone lysine methyltransferase inhibitor
- A4166 EPZ56761 CitationTarget: DOT1LSummary: DOT1L inhibitor,potent and SAM competitive
- A4168 EntacaponeTarget: Catechol O-Methyltransferase (COMT)Summary: COMT inhibitor
- A4170 EPZ004777Target: DOT1LSummary: DOT1L inhibitor