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.
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A4546 Mithramycin ASummary: Anticancer antibiotic -
A4547 ThiolutinSummary: RNA polymerase inhibitor,antibiotic -
A4489 TC-A 2317 hydrochlorideTarget: Aurora KinasesSummary: Aurora kinase A inhibitor,potent and selective -
A4490 I-CBP 112Target: CREBBP|EP300Summary: CBP/EP300 bromodomain inhibitor -
A4491 SGC-CBP302 CitationTarget: CREBBP|EP300Summary: Inhibitor of CREBBP/EP300 bromodomain,potent -
A4492 NU 90562 CitationTarget: Histone Acetyltransferases (HATs)Summary: KAT5 (Tip60) HAT inhibitor -
A4494 LMK 235Summary: HDAC4/HDAC5 inhibitor -
A4498 SBHA1 CitationTarget: Histone Deacetylases (HDACs)Summary: HDAC1/HDAC3 inhibitor,cell-permeable -
A4503 UNC 0224Summary: G9a histone methyltransferase inhibitor -
A4506 DMOG4 CitationTarget: Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors (HIF-PHIs)Summary: Competitive HIF-PH inhibitor, cell-permeable

