Chromatin/Epigenetics - HIV - Myeloma - Neuroblastoma - Colorectal Cancer
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.
- B5916 Chidamide1 CitationTarget: HDACSummary: HDAC抑制剂
- B1013 GSK1324726ATarget: BromodomainsSummary: BET蛋白抑制剂
- A1912 Lomeguatrib中文名: 罗米鲁曲Target: O6-methylguanine-DNA-methyl-transferase (MGMT)Summary: MGMT抑制剂
- A4186 Bromosporine1 CitationTarget: BromodomainsSummary: Bromodomain抑制剂
- A4126 Aurora A Inhibitor I中文名: 极光A抑制剂ITarget: Aurora KinasesSummary: Aurora A抑制剂
- A4099 Valproic acid sodium salt (Sodium valproate)中文名: 丙戊酸钠Target: Histone Deacetylases (HDACs)Summary: HDAC抑制剂
- A4111 VX-680 (MK-0457,Tozasertib)中文名: 陶扎色替Target: Aurora KinasesSummary: Aurora 激酶抑制剂
- A8173 Romidepsin (FK228, depsipeptide)7 Citation中文名: 罗米地辛Target: Histone Deacetylases (HDACs)Summary: 选择性的HDAC1/HDAC2抑制剂
- A8178 Panobinostat (LBH589)10 Citation中文名: 帕比司他Target: Histone Deacetylases (HDACs)Summary: HDAC抑制剂
- A8171 Entinostat (MS-275,SNDX-275)2 Citation中文名: 恩替诺特Target: Histone Deacetylases (HDACs)Summary: HDAC1和HDAC3抑制剂