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.
- B5607 IOX 11 CitationSummary: histone demethylase JMJD inhibitor
- B5670 I-BET 151 hydrochloride1 CitationSummary: BET bromodomain inhibitor
- B5685 GSK J2Summary: inactive control of GSK J1, JMJD3 (KDM6B) and UTX (KDM6A) inhibitor
- B5686 GSK J5Summary: inactive isomer of GSK J4, KDM inhibitor
- B5798 TC-E 5001Summary: dual tankyrase (TNKS) inhibitor
- A8893 Rucaparib (free base)Target: PARPSummary: Potent PARP inhibitor
- B8023 Cerdulatinib (PRT062070)Target: JAK|Syk|TYK2Summary: Syk/JAK inhibitor
- B4875 PFI-21 CitationTarget: SETD7Summary: SETD7 methyltransferase inhibitor
- B4887 RemodelinTarget: NAT10Summary: NAT10 inhibitor
- B4846 LB-100Summary: protein phosphatase 2A(PP2A)inhibitor