Chromatin/Epigenetics - Lck - PI3K - Histone Acetyltransferases (HATs) - Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors (HIF-PHIs)
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.
- A4506 DMOGTarget: Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors (HIF-PHIs)Summary: 细胞通透的竞争性HIF-PH抑制剂
- A4492 NU 9056Target: Histone Acetyltransferases (HATs)Summary: KAT5(Tip60)HAT抑制剂
- A4488 Anacardic acid中文名: 漆树酸Target: Histone Acetyltransferases (HATs)Summary: HAT抑制剂
- A4097 CUDC-907中文名: 非美诺司他Target: Histone Deacetylases (HDACs)|PI3KSummary: PI3K/HDAC抑制剂
- A4113 ZM 447439Target: Aurora Kinases|MEK|Src|LckSummary: Aurora激酶抑制剂