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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B5980 CHZ8681 CitationSummary: Type II JAK2 inhibitor -
B5998 GSK2801Summary: inhibitor of BAZ2A and BAZ2B bromodomains -
B6004 PX-478 2HCl6 CitationTarget: Hypoxia Inducible Factors (HIFs)Summary: HIF-1α inhibitor -
B6005 Peficitinb (ASP015K, JNJ-54781532)Summary: JAK inhibitor -
B6014 BI-847325Summary: dual inhibitor of MEK and Aurora kinases -
B6016 SirReal2Summary: Sirt2 inhibitor -
A8725 UNC3866Summary: a potent antagonist of CBX4 and CBX7 chromodomains -
B6048 SGC707Summary: PRMT3 inhibitor -
B6091 GSK-J1 sodium salt1 Citation -
B7796 OxamflatinSummary: HADC inhibitor

