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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A4495 NCH 51Summary: Histone deacetylase (HDAC) inhibitor -
A4510 1,2,3,4,5,6-HexabromocyclohexaneSummary: JAK2 tyrosine kinase inhibitor -
B1164 MK-4827 tosylateSummary: PARP1/PARP2 inhibitor -
B6014 BI-847325Summary: dual inhibitor of MEK and Aurora kinases -
B6048 SGC707Summary: PRMT3 inhibitor -
C4401 PTP Inhibitor IVSummary: PTP inhibitor -
B7744 PFI 3Target: Protein polybromo-1|SMARCA4|SMARCA2Summary: inhibitor of polybromo 1 and SMARCA4 -
A4494 LMK 235Summary: HDAC4/HDAC5 inhibitor -
A8807 MK-8745Target: Aurora KinasesSummary: Aurora A inhibitor,potent and selective -
B1163 MK-4827 hydrochlorideSummary: PARP1/PARP2 inhibitor
