Chromatin/Epigenetics - KDM - MDM2 - FGFR - Src
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.
- A8712 MCB-613Target: SrcSummary: 类固醇受体共激活因子(SRC)刺激物
- B4930 TC-E 5002Target: KDMSummary: 选择性组蛋白去甲基化酶KDM2/7亚家族抑制剂
- A3348 Daminozide中文名: 丁酰肼Target: KDM|PHFSummary: KDM2A抑制剂
- A4124 TAK-901Target: Aurora Kinases|FLT3|Src|JAK|LRRK2|Hck|FGR|YES|Fyn|ARGSummary: Aurora A/B抑制剂
- A4122 PHA-680632Target: Aurora Kinases|PLK|FGFRSummary: Aurora激酶抑制剂
- A4130 ENMD-2076Target: Aurora Kinases|FLT3|RET|Src|VEGFR3/FLT4|NTRK1/TRKA|CSF-1R/c-FmsSummary: Aurora A/Flt3的选择性抑制剂
- A4113 ZM 447439Target: Aurora Kinases|MEK|Src|LckSummary: Aurora激酶抑制剂
- A4150 WHI-P154Target: VEGFR|Src|EGFR|JAKSummary: JAK3抑制剂
- A4147 LY2784544Target: Aurora Kinases|FLT3|VEGFR|FGFR|Trk Receptors|JAK|ALK|TYK2|MUSK|MAP3KSummary: JAK2抑制剂
- N1315 Parthenolide中文名: 小白菊内酯,欧苷菊Target: Histone Deacetylases (HDACs)|MDM2|DNA Methyltransferases|p53|5-HT