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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BA2908 KaranjinSummary: Karanjin is an orally active furanoflavonoid that can be isolated from several legumes. -
BA2996 UC-514321Summary: A selective TET1 inhibitor -
BA3362 RK-9123016Summary: RK-9123016 is a potent inhibitor. -
BA3950 SF2523Summary: A potent and selective inhibitor. -
BA4115 SE-7552Summary: SE-7552, a 2-(difluoromethyl)-1,3,4-oxadiazole (DFMO) derivative, is an orally active, highly selective, non-isohydroxamic acid inhibitor. -
BA4118 FT895Summary: FT895 is a potent and selective inhibitor. -
BA4119 CorinSummary: Corin is a dual inhibitor of histidine lysine-specific demethylase and histidine deacetylase. -
BA4122 GivinostatSummary: Inhibitors. -
BA4128 TYA-018Summary: TYA-018 is an orally effective and highly selective inhibitor. -
BA4130 SR-4370Summary: An effective inhibitor.

