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.
- A8712 MCB-613Target: SrcSummary: stimulator of steroid receptor coactivator (SRC)
- B5879 GSK28795521 CitationTarget: LSDSummary: Novel and irreversible LSD1 inhibitor
- B5916 Chidamide1 CitationTarget: HDACSummary: Novel HDAC inhibitor
- B6004 PX-478 2HClTarget: Hypoxia Inducible Factors (HIFs)Summary: HIF-1α inhibitor
- B1012 MS436Target: BromodomainsSummary: BRD4 inhibitor
- B1013 GSK1324726ATarget: BromodomainsSummary: BET proteins inhibitor
- B1255 AZ505Target: SMYD2Summary: SMYD2 inhibitor,potent and selective
- B1115 BAY 87-2243Target: Hypoxia Inducible Factors (HIFs)Summary: HIF-1 inhibitor,potent and selective
- B1182 ABC294640Target: SKSummary: Sphingosine kinase 2 inhibitor,selective and competitive
- B1577 C6461 CitationTarget: p300Summary: HAT p300-CBP inhibitor,cell-permeable