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.
- C4119 2',3',5'-triacetyl-5-AzacytidineSummary: DNA甲基转移酶抑制剂5-azacytidine的前药形式
- C4247 RN-1 (hydrochloride)Summary: LSD1抑制剂
- C4229 UMB-32Summary: BET溴结构域BRD4和含有溴结构域的转录因子TAF1和TAF1L的抑制剂
- C4018 4-iodo-SAHASummary: I类和II类组蛋白去乙酰化酶(HDAC)抑制剂
- C4097 NI-57Summary: BRPF蛋白溴结构域的抑制剂
- C3776 MS049 (hydrochloride)Summary: PRMT4和PRMT6抑制剂
- C3829 Cl-Amidine (trifluoroacetate salt)Summary: PAD4脱氨活性抑制剂
- C3668 GSK6853Summary: BRPF1抑制剂
- C3996 PRL-3 InhibitorSummary: 再生肝脏蛋白磷酸酶-3(PRL-3)抑制剂
- C3823 Phthalazinone pyrazoleSummary: Aurora A激酶抑制剂