Chromatin/Epigenetics - Acute Myeloid Leukemia - Cancer
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.
- A3962 AZD1208Target: PimSummary: PIM激酶抑制剂
- A3958 Veliparib dihydrochloride中文名: 维利帕尼二盐酸盐Target: PARPSummary: PARP-1/PARP-2抑制剂
- A3937 XL019Target: JAKSummary: 有效的JAK2选择性抑制剂
- 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
- A3556 LKB1 (AAK1 dual inhibitor)Target: PimSummary: Pim-1激酶抑制剂
- A3214 AZD11521 CitationTarget: Aurora KinasesSummary: Aurora B激酶抑制剂
- A1915 Zebularine1 Citation中文名: 泽布拉林Target: DNA Methyltransferases|Cytidine deaminasesSummary: DNA甲基化抑制剂
- A1913 RG 1083 CitationTarget: DNA MethyltransferasesSummary: DNA甲基转移酶抑制剂
- A1912 Lomeguatrib中文名: 罗米鲁曲Target: O6-methylguanine-DNA-methyl-transferase (MGMT)Summary: MGMT抑制剂