Chromatin/Epigenetics - Selective - PI3K - Aurora Kinases - NAT10
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.
- B4887 RemodelinTarget: NAT10Summary: NAT10抑制剂
- A8807 MK-8745Target: Aurora KinasesSummary: Aurora A的强效选择性抑制剂。
- A4489 TC-A 2317 hydrochlorideTarget: Aurora KinasesSummary: Aurora kinase A抑制剂
- A3760 Reversine中文名: 逆转素Target: Aurora KinasesSummary: Aurora激酶抑制剂
- A3214 AZD11521 CitationTarget: Aurora KinasesSummary: Aurora B激酶抑制剂
- A4128 PF-03814735Target: Aurora KinasesSummary: Aurora A/B抑制剂
- A4127 GSK1070916Target: Aurora KinasesSummary: Aurora B/C抑制剂
- A4126 Aurora A Inhibitor I中文名: 极光A抑制剂ITarget: Aurora KinasesSummary: Aurora A抑制剂
- A4118 Hesperadin1 Citation中文名: 橙皮甙,橙皮苷Target: Aurora KinasesSummary: Aurora B抑制剂
- A4115 JNJ-77066211 CitationTarget: Cyclin-Dependent Kinases|Aurora KinasesSummary: 有效的CDK/Aurora抑制剂