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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A8221 EPZ-64389 CitationSummary: EZH2 inhibitor -
A8223 CID 2011756Summary: PKD inhibitor -
A8242 SplitomicinSummary: inhibitor of Sir2p and fMLP-induced free radicals -
A1877 XAV-93916 CitationTarget: TNKSSummary: Tankyrase 1/2 (TNKS) inhibitor -
A3002 ABT-888 (Veliparib)9 CitationSummary: Potent PARP inhibitor -
A3012 Ruxolitinib (INCB018424)12 CitationTarget: JAKSummary: JAK1 and JAK2 inhibitor -
A4083 Rocilinostat (ACY-1215)1 CitationTarget: Histone Deacetylases (HDACs)Summary: Selective HDAC6 inhibitor -
A4089 Mocetinostat (MGCD0103, MG0103)4 CitationTarget: Histone Deacetylases (HDACs)Summary: HDAC inhibitor,isotype-selective and potent -
A4090 JNJ-264815853 CitationTarget: Histone Deacetylases (HDACs)Summary: Potent HDAC inhibitor -
A4091 PCI-340511 CitationTarget: Histone Deacetylases (HDACs)Summary: HDAC8 inhibitor,potent and selective

