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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A1909 BIX 012942 CitationTarget: G9aSummary: G9a and GLP inhibitor -
A1910 Bromodomain Inhibitor, (+)-JQ169 CitationTarget: BromodomainsSummary: BET bromodomain inhibitor -
A1913 RG 1083 CitationTarget: DNA MethyltransferasesSummary: DNA methyltransferase inhibitor -
A3958 Veliparib dihydrochlorideTarget: PARPSummary: PARP-1/PARP-2 inhibitor -
A3962 AZD1208Target: PimSummary: PIM kinase inhibitor -
A4488 Anacardic acid1 CitationTarget: Histone Acetyltransferases (HATs)Summary: HAT inhibitor -
A4493 KD 51701 CitationSummary: HDAC inhibitor -
A4495 NCH 51Summary: Histone deacetylase (HDAC) inhibitor -
A4496 NSC 3852Target: Histone Deacetylases (HDACs)Summary: HDAC inhibitor -
A4497 PyroxamideTarget: Histone Deacetylases (HDACs)Summary: HDAC1 inhibitor

