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.
- A4166 EPZ56761 CitationTarget: DOT1LSummary: DOT1L inhibitor,potent and SAM competitive
- A4171 EPZ0056872 CitationTarget: EZH2Summary: EZH2 inhibitor,potent and selective
- A4170 EPZ004777Target: DOT1LSummary: DOT1L inhibitor
- B4989 EPZ015666Target: Protein Arginine MethyltransferasesSummary: PRMT5 inhibitor
- A8182 3-Deazaneplanocin A (DZNep) hydrochloride1 CitationTarget: EZH2Summary: SAHH and EZH2 inhibitor
- B1581 EPZ004777 HClTarget: DOT1LSummary: DOT1L inhibitor,potent and selective
- B1255 AZ505Target: SMYD2Summary: SMYD2 inhibitor,potent and selective
- A8221 EPZ-64385 CitationSummary: EZH2 inhibitor, potent and selective