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.
- B5959 GSK J4 free baseSummary: histone demethylase JMJD3/UTX inhibitor
- B5861 Molidustat (BAY85-3934)Target: HIF-PHSummary: Novel HIF-PH inhibitor
- B5879 GSK28795521 CitationTarget: LSDSummary: Novel and irreversible LSD1 inhibitor
- B5913 C7280948Summary: Novel PRMT1 inhibitor
- B5916 Chidamide1 CitationTarget: HDACSummary: Novel HDAC inhibitor
- B5929 Decernotinib(VX-509)Summary: Selective and orally active JAK3 inhibitor
- B5936 ACY-241Summary: Selective and orally active HDAC6 inhibitor
- B5949 BG45Summary: Novel HDAC3-selective inhibitor
- B5967 UF 010Summary: Novel and selective class I HDAC inhibitor
- B5968 BML-210(CAY10433)Summary: Novel HDAC inhibitor