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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BA2777 NU9056Summary: NU9056 is a potent and selective histone acetyltransferase inhibitor. -
BA2779 PROTAC-O4I2Summary: PROTAC-O4I2 is a target of splicing factor 3B1. -
BA2805 DecursinSummary: Decursin ((+)-Decursin) is a potent antitumor agent. -
BA2807 UNC0321Summary: UNC0321 is a potent and selective histone methyltransferase inhibitor. -
BA2813 TH1834Summary: TH1834 is a specific histone acetyltransferase inhibitor. -
BA2814 SKLB325Summary: SKLB325 is an inhibitor. -
BA2831 MRT199665Summary: MRT199665 is a potent, ATP-competitive, selective inhibitor. -
BA2834 JQAD1Summary: JQAD1 is CRBN-dependent and selectively targeted for degradation. -
BA2848 Wu-5Summary: Wu-5 is a USP10 inhibitor. -
BA2858 MC4033Summary: MC4033 is a selective, reversible inhibitor of lysine acetyltransferase 8.

