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.
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A4186 Bromosporine1 CitationTarget: BromodomainsSummary: Bromodomain inhibitor,non-selective -
A1905 3-Deazaneplanocin,DZNep6 CitationTarget: HydrolaseSummary: S-adenosylhomocysteine and EZH2 inhibitor -
A1906 Decitabine (NSC127716, 5AZA-CdR)4 CitationSummary: Deoxycytidine analog and cellular diifferentiation inducer -
A1907 5-Azacytidine11 CitationTarget: DNA MethyltransferasesSummary: DNA methyltransferase inhibitor. -
A1908 AMI-1Summary: PRMT1 inhibitor -
A1912 LomeguatribTarget: O6-methylguanine-DNA-methyl-transferase (MGMT)Summary: MGMT inhibitor -
A1914 UNC06381 CitationSummary: G9a/GLP HMTase inhibitor, potent and selective -
A1915 Zebularine1 CitationTarget: DNA Methyltransferases|Cytidine deaminasesSummary: Cytidine analog; DNA methyltransferase (DNMT) inhibitor; induces DNA demethylation -
A1146 Histone-H2A-(107-122)-Ac-OHSummary: Histone-H2A peptide -
A3214 AZD11521 CitationTarget: Aurora KinasesSummary: Aurora B kinase inhibitor,highly potent and selective

