Chromatin/Epigenetics - Multiple Myeloma - Hepatocellular Carcinoma - Cervical Cancer - Diffuse Large B-cell Lymphoma
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.
- A3760 Reversine中文名: 逆转素Target: Aurora KinasesSummary: Aurora激酶抑制剂
- A3692 OTX-0153 Citation中文名: 比拉瑞塞Target: BromodomainsSummary: BRD抑制剂
- A1907 5-Azacytidine6 Citation中文名: 氮胞苷(5-氮胞苷)Target: DNA MethyltransferasesSummary: DNA甲基转移酶抑制剂
- A4186 Bromosporine1 CitationTarget: BromodomainsSummary: Bromodomain抑制剂
- A4093 ITF2357 (Givinostat)2 CitationTarget: Histone Deacetylases (HDACs)Summary: HDAC抑制剂
- A4083 Rocilinostat (ACY-1215)1 CitationTarget: Histone Deacetylases (HDACs)Summary: 选择性的HDAC6抑制剂
- A8178 Panobinostat (LBH589)10 Citation中文名: 帕比司他Target: Histone Deacetylases (HDACs)Summary: HDAC抑制剂