CK2-mediated phosphorylation of SUZ12 promotes PRC2 …
2022年11月9日 · Here the authors identify SUZ12 as a cellular substate of casein kinase 2 (CK2), and show this phosphorylation changes the active site structure of Polycomb repressive complex 2 (PRC2) and ...
Structure of the PRC2 complex and application to drug discovery
2017年4月17日 · PRC2 catalyzes the methylation of histone H3 lysine 27 (H3K27) through its EZH2 subunit, a modification thought to mediate transcriptional silencing through chromatin compaction 1, 10.
An EED/PRC2-H19 Loop Regulates Cerebellar Development
2 天之前 · EED (embryonic ectoderm development) is a core subunit of the polycomb repressive complex 2 (PRC2), which senses the trimethylation of histone H3 lysine 27 (H3K27). ... Loss of function variants in individual PRC2 subunits, EED, SUZ12, or EZH2, causes human Cohen- Gibson or Weaver-like syndrome, a rare congenital disorder characterized by ...
生命学院戚炜团队揭示PRC2抑制剂抗肿瘤机理 - ShanghaiTech
2022年2月17日 · PRC2（Polycomb Repressive Complex 2，多梳抑制复合体2）是重要的表观修饰酶，核心亚基包括EZH2、EED和SUZ12，可对组蛋白H3的27位赖氨酸K27进行甲基化修饰，具有转录抑制的作用。
EZH2 variants differentially regulate polycomb repressive complex 2 …
Our previous results demonstrate that EED, EZH2, and SUZ12 are dramatically upregulated in pachytene spermatocytes , suggesting the germ cell-specific PRC2 complex has a role in establishing H3K27 methylation during meiotic progression. Therefore, it is crucial to understand how PRC2 can distinguish these two different types of histone ...
EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 …
2020年1月16日 · Our PROTACs bind to EED (pK D ∼ 9.0) and promote ternary complex formation with the E3 ubiquitin ligase. The PROTACs potently inhibit PRC2 enzyme activity (pIC 50 ∼ 8.1) and induce rapid degradation of not only EED but also EZH2 and SUZ12 within the
Targeting EED as a key PRC2 complex mediator toward novel …
2024年6月1日 · PRC2 complex comprises enhancer of zeste homolog 2 (EZH2) or enhancer of zeste homolog 1 (EZH1), embryonic ectoderm development (EED), and suppressor of zeste 12 protein homolog (SUZ12). EZH2, functioning as a histone methyltransferase (HMTase), interacts with EED and SUZ12 to catalyze the transfer of a methyl group from the cofactor S ...
LINE1 and PRC2 control nucleolar organization and ... - Cell Press
2024年10月15日 · We found that LINE1 RNA associates with EZH2 and SUZ12, components of the PRC2 complex that deposits H3K27me3, in RSeT + DT hESCs (Figure 5E). Moreover, chemical inhibition of PRC2 (PRC2i) using the EZH2 inhibitor UNC1999 41 induces transcriptional changes similar to those induced by LINE1 KD, including the upregulation of the 8C program ...
Binding Interactions between Long Noncoding RNA HOTAIR and PRC2 …
The PRC2 complex contains the three core protein subunits EZH2, EED, and SUZ12. EZH2 contains a SET domain which catalyzes trimethylation of histone H3 at lysine 27 (H3K27 → H3K27Me3), a mark associated with transcriptional repression; SUZ12 and EED are also required for this EZH2 methyltransferase activity to occur. 6 The core PRC2 complex ...
EZH2: biology, disease, and structure-based drug discovery
2013年12月23日 · EZH2 is the catalytic subunit of the polycomb repressive complex 2 (PRC2), which is a highly conserved histone methyltransferase that methylates lysine 27 of histone 3. Overexpression of...
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