Chromatin/Epigenetics - Acute Myeloid Leukemia
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.
- B4894 SP2509Target: Histone DemethylasesSummary: 新型LSD1拮抗剂
- A4490 I-CBP 112Target: CREBBP|EP300Summary: CBP/EP300 bromodomain抑制剂
- A3962 AZD1208Target: PimSummary: PIM激酶抑制剂
- A3760 ReversineTarget: Aurora KinasesSummary: Aurora激酶抑制剂
- A3692 OTX-0153 CitationTarget: BromodomainsSummary: BRD抑制剂
- A1905 3-Deazaneplanocin,DZNep6 CitationTarget: HydrolaseSummary: S-腺苷高半胱氨酸和EZH2抑制剂。
- A4112 Barasertib (AZD1152-HQPA)3 CitationTarget: Aurora KinasesSummary: Aurora Kinase B抑制剂
- A3012 Ruxolitinib (INCB018424)4 CitationTarget: JAKSummary: JAK抑制剂
- A8182 3-Deazaneplanocin A (DZNep) hydrochloride1 CitationTarget: EZH2Summary: SAHH和EZH2抑制剂