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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BA2814 SKLB325Summary: SKLB325 is an inhibitor. - BA2831 MRT199665Summary: MRT199665 is a potent, ATP-competitive, selective inhibitor.
- BA2834 JQAD1Summary: JQAD1 is CRBN-dependent and selectively targeted for degradation.
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BA2848 Wu-5Summary: Wu-5 is a USP10 inhibitor. - BA2858 MC4033Summary: MC4033 is a selective, reversible inhibitor of lysine acetyltransferase 8.
- BA2859 BJE6-106Summary: BJE6-106 (B106) is a potent and selective inhibitor.
- BA2863 WDR5-IN-1Summary: WDR5-IN-1 is a potent and selective WD repeat structural domain 5 inhibitor.
- BA2874 NHWD-870Summary: NHWD-870 is a potent, orally active and selective inhibitor.
- BA2875 BETd-260Summary: BETd-260 (ZBC260), a PROTAC linked by ligand and ligand-conjugated, was able to reduce protein activity at a low concentration of 30 pM in leukemia cells RS4;11.
- BA2908 KaranjinSummary: Karanjin is an orally active furanoflavonoid that can be isolated from several legumes.