Chromatin/Epigenetics - Acute Myeloid Leukemia - Myelofibrosis - Colon Cancer - Dyskinesia - Diabetes
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.
- A3214 AZD11521 CitationTarget: Aurora KinasesSummary: Aurora B激酶抑制剂
- A1913 RG 1083 CitationTarget: DNA MethyltransferasesSummary: DNA甲基转移酶抑制剂
- 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。
- A4128 PF-03814735Target: Aurora KinasesSummary: Aurora A/B抑制剂
- A4127 GSK1070916Target: Aurora KinasesSummary: Aurora B/C抑制剂
- A4098 PCI-24781 (CRA-024781)Target: Histone Deacetylases (HDACs)Summary: Pan-HDAC抑制剂
- A4112 Barasertib (AZD1152-HQPA)3 Citation中文名: 巴拉塞替Target: Aurora KinasesSummary: Aurora Kinase B抑制剂
- A4182 Resveratrol2 Citation中文名: 白藜芦醇Target: Sir2-like Family Deacetylases (Sirtuins)|COX|LOX|Adenylyl cyclase|Quinone reductaseSummary: SIRT1激活剂
- A4136 TG101348 (SAR302503)2 Citation中文名: 费德拉替尼Target: FLT3|JAK|c-RETSummary: JAK-2抑制剂
- A4090 JNJ-264815853 CitationTarget: Histone Deacetylases (HDACs)Summary: HDAC抑制剂