Chromatin/Epigenetics - Type 2 Diabetes - Non-small Cell Lung Cancer - Myeloma - Immunological Diseases
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.
- B1115 BAY 87-2243Target: Hypoxia Inducible Factors (HIFs)Summary: 有效的HIF-1选择性抑制剂
- A3821 SRT2104 (GSK2245840)1 CitationTarget: Sir2-like Family Deacetylases (Sirtuins)Summary: SIRT1激活剂
- A3692 OTX-0153 Citation中文名: 比拉瑞塞Target: BromodomainsSummary: BRD抑制剂
- A4102 CI994 (Tacedinaline)1 Citation中文名: 乙酰地那林,他地那兰Target: Histone Deacetylases (HDACs)Summary: HDAC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
- A4097 CUDC-907中文名: 非美诺司他Target: Histone Deacetylases (HDACs)|PI3KSummary: PI3K/HDAC抑制剂
- A4180 SRT1720 HCl3 CitationTarget: Sir2-like Family Deacetylases (Sirtuins)Summary: SIRT1激活剂
- A4138 Tofacitinib (CP-690550,Tasocitinib)1 Citation中文名: 托法替尼,托法替布Target: JAKSummary: Janus激酶抑制剂
- 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