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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A4160 A-966492Target: PARPSummary: PARP-1/-2 inhibitor, highly potent -
A4117 AT9283Summary: Aurora kinase/JAK inhibitor -
A3937 XL019Target: JAKSummary: JAK2 inhibitor,potent and selective -
A4502 ChaetocinSummary: SUV39H1 Inhibitor -
A4542 Alexidine dihydrochlorideSummary: PTPMT1 inhibitor; PLB inhibitor -
B4983 GSK-LSD1 2HClSummary: irreversible, and selective LSD1 inhibitor -
B6004 PX-478 2HCl6 CitationTarget: Hypoxia Inducible Factors (HIFs)Summary: HIF-1α inhibitor -
B1012 MS436Target: BromodomainsSummary: BRD4 inhibitor -
B4713 AK-7Summary: selective and brain-permeable SIRT2 inhibitor -
B7250 YM 750Summary: Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor
