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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A4097 CUDC-907Target: Histone Deacetylases (HDACs)|PI3KSummary: Potent PI3K/HDAC inhibitor -
A4121 SNS-314 MesylateTarget: Aurora KinasesSummary: Aurora A/B/C kinases inhibitor, potent and selective -
A8221 EPZ-64385 CitationSummary: EZH2 inhibitor -
A8223 CID 2011756Summary: PKD inhibitor -
B1499 RVX-2082 CitationSummary: Potent BET bromodomain inhibitor -
B5879 GSK28795521 CitationTarget: LSDSummary: Novel and irreversible LSD1 inhibitor -
C3209 Butyrolactone 31 CitationSummary: histone acetyltransferase Gcn5 inhibitor -
B7594 SalermideSummary: SIRT1 and SIRT2 inhibitor -
A4137 AZD1480Target: JAKSummary: JAK2 inhibitor,ATP-competitive and novel -
A4164 AZD2461Target: PARPSummary: Novel PARP inhibitor
