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.
- N1315 ParthenolideTarget: Histone Deacetylases (HDACs)|MDM2|DNA Methyltransferases|p53|5-HT
- B3393 MK-4827 RacemateSummary: selective inhibitor of PARP1/PARP2
- B3704 Nexturastat ATarget: Histone Deacetylases (HDACs)Summary: HDAC6 inhibitor,highly potent and selective
- B4106 4SC-202Summary: Class I HDAC inhibitor
- B4655 BMS-345541(free base)Summary: IKK-1/IKK-2 inhibitor,potent and selective
- B4713 AK-7Summary: selective and brain-permeable SIRT2 inhibitor
- B6881 NSC 6632841 CitationSummary: Cdc25 dual specificity phosphatases inhibitor
- B7009 TautomycetinSummary: A novel and specific protein phosphatase 1 (PP1) inhibitor
- B7514 Tranylcypromine hydrochloride1 CitationSummary: Monoamine oxidase inhibitor
- B7744 PFI 3Target: Protein polybromo-1|SMARCA4|SMARCA2Summary: inhibitor of polybromo 1 and SMARCA4