Chromatin/Epigenetics - G9a - Lck - L3MBTL - EP300
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.
- B7757 UNC 0642Target: G9a|GLPSummary: G9a和GLP组蛋白赖氨酸甲基转移酶抑制剂
- A4491 SGC-CBP302 CitationTarget: CREBBP|EP300Summary: CREBBP/EP300 bromodomain抑制剂
- A4490 I-CBP 112Target: CREBBP|EP300Summary: CBP/EP300 bromodomain抑制剂
- A3901 UNC12151 CitationTarget: L3MBTLSummary: 甲基赖氨酸的化学探针
- A1909 BIX 01294Target: G9aSummary: G9a和GLP抑制剂
- A4113 ZM 447439Target: Aurora Kinases|MEK|Src|LckSummary: Aurora激酶抑制剂