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.
-   B1583 UNC19992 CitationTarget: EZH2|EZH1Summary: EZH2 inhibitor B1583 UNC19992 CitationTarget: EZH2|EZH1Summary: EZH2 inhibitor
-   B4918 OXF BD 02Summary: Selective inhibitor of the first bromodomain of BRD4 B4918 OXF BD 02Summary: Selective inhibitor of the first bromodomain of BRD4
-   B5970 Sanguinarine chlorideSummary: Inhibitor of PP2C and MKP-1 B5970 Sanguinarine chlorideSummary: Inhibitor of PP2C and MKP-1
-   C3584 PBITSummary: JARID1 family demethylases inhibitor C3584 PBITSummary: JARID1 family demethylases inhibitor
-   A4145 TG101209Summary: JAK2/3 inhibitor A4145 TG101209Summary: JAK2/3 inhibitor
-   A4103 LAQ824 (NVP-LAQ824,Dacinostat)1 CitationSummary: HDAC inhibitor,potent and novel A4103 LAQ824 (NVP-LAQ824,Dacinostat)1 CitationSummary: HDAC inhibitor,potent and novel
-   A4127 GSK1070916Target: Aurora KinasesSummary: Aurora B/C inhibitor A4127 GSK1070916Target: Aurora KinasesSummary: Aurora B/C inhibitor
-   A4528 EB 47Summary: Potent PARP-1 inhibitor A4528 EB 47Summary: Potent PARP-1 inhibitor
-   B1582 MM-1021 CitationSummary: MLL1 inhibitor,high-affinity peptidomimetic B1582 MM-1021 CitationSummary: MLL1 inhibitor,high-affinity peptidomimetic
-   B4846 LB-100Summary: protein phosphatase 2A(PP2A)inhibitor B4846 LB-100Summary: protein phosphatase 2A(PP2A)inhibitor
