Chromatin/Epigenetics - Pim - PARP - Bromodomains
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.
- A8893 Rucaparib (free base)中文名: 瑞卡帕布Target: PARPSummary: PARP抑制剂
- B1013 GSK1324726ATarget: BromodomainsSummary: BET蛋白抑制剂
- B1012 MS436Target: BromodomainsSummary: BRD4抑制剂
- B1498 I-BET-7624 CitationTarget: BromodomainsSummary: BET抑制剂
- A8808 ME0328Target: PARPSummary: PARP抑制剂
- A3962 AZD1208Target: PimSummary: PIM激酶抑制剂
- A3958 Veliparib dihydrochloride中文名: 维利帕尼二盐酸盐Target: PARPSummary: PARP-1/PARP-2抑制剂
- A3729 PJ34Target: PARPSummary: PARP-1抑制剂
- A3692 OTX-0153 Citation中文名: 比拉瑞塞Target: BromodomainsSummary: BRD抑制剂
- A3617 MK-4827中文名: 尼拉帕尼Target: PARPSummary: PARP-1/-2抑制剂