Chromatin/Epigenetics - Acute Myeloid Leukemia - Lymphoma - Hepatocellular Carcinoma - Neuroblastoma
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.
- B4989 EPZ015666Target: Protein Arginine MethyltransferasesSummary: PRMT5抑制剂
- B4894 SP2509Target: Histone DemethylasesSummary: 新型LSD1拮抗剂
- B8023 Cerdulatinib (PRT062070)Target: JAK|Syk|TYK2Summary: Syk/JAK抑制剂
- B1013 GSK1324726ATarget: BromodomainsSummary: BET蛋白抑制剂
- A8803 RGFP9664 CitationTarget: Histone Deacetylases (HDACs)Summary: HDAC3抑制剂
- A4490 I-CBP 112Target: CREBBP|EP300Summary: CBP/EP300 bromodomain抑制剂
- A3962 AZD1208Target: PimSummary: PIM激酶抑制剂
- 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
- A1905 3-Deazaneplanocin,DZNep6 Citation中文名: 3-去氮腺嘌呤ATarget: HydrolaseSummary: S-腺苷高半胱氨酸和EZH2抑制剂。