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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A4100 Droxinostat2 CitationSummary: Selective HDAC inhibitor -
A4124 TAK-901Target: Aurora Kinases|FLT3|Src|JAK|LRRK2|Hck|FGR|YES|Fyn|ARGSummary: Novel Aurora A/B inhibitor -
A4525 BYK 204165Summary: PARP-1 inhibitor,potent and selective -
B4895 OF-1Summary: BRPF1B and BRPF2 bromodomain inhibitor -
C5773 CTPBSummary: selective activator of the histone acetyltransferase (HAT) p300 -
B6084 AS8351Summary: histone demethylase inhibitor -
C3888 JGB1741Summary: SIRT1 inhibitor -
B1255 AZ505Target: SMYD2Summary: SMYD2 inhibitor,potent and selective -
B1177 NafamostatSummary: Broad spectrum serine protease inhibitor, kallikrein inhibitor -
A4140 WP1066Target: STAT|JAKSummary: JAK2/STAT3 inhibitor,cell-permeable
