Chromatin/Epigenetics - Tankyrases - JAK - Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors (HIF-PHIs) - PTP
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.
- B8023 Cerdulatinib (PRT062070)Target: JAK|Syk|TYK2Summary: Syk/JAK抑制剂
- B1130 GLPG06341 Citation中文名: 菲戈替尼Target: JAKSummary: JAK1抑制剂
- A8601 Tankyrase Inhibitors (TNKS) 49Target: TankyrasesSummary: 端锚聚合酶抑制剂
- A4506 DMOGTarget: Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors (HIF-PHIs)Summary: 细胞通透的竞争性HIF-PH抑制剂
- A4544 NSC 87877Target: PTPSummary: Shp2/Shp1 PTP抑制剂
- A4512 Cucurbitacin I中文名: 葫芦素 ITarget: STAT|JAKSummary: STAT3/JAK2信号转导抑制剂
- A4511 Cercosporamide中文名: 尾孢素酰胺Target: JAK|MNKSummary: Mnk2和JAK3抑制剂
- A3937 XL019Target: JAKSummary: 有效的JAK2选择性抑制剂
- A3741 Pyridone 6中文名: 吡啶酮6Target: JAKSummary: Pan-JAK抑制剂
- A4152 BMS-911543Target: JAKSummary: JAK2抑制剂