2021年1月29日 · Overall, PRC2:EZH1 displays the expected bipartite structure with an upper catalytic lobe containing EZH1, EED, and the C-terminal VEFS domain of SUZ12, and a lower regulatory lobe containing...

PRC2是一种多蛋白转录抑制复合物，包含四个核心成分: EZH2及其高度相关的同源物EZH1、胚胎外胚层发育的抑制子(EED)、zeste 12的抑制子(SUZ12)和视网膜母细胞肿瘤相关蛋白46和48 (RbAp46/48) (图1)。

三甲基化jarid2蛋白可以与eed 结合并变构刺激prc2甲基转移酶活性，这一发现促使药物化学家尝试设计eed顶腔结合剂以抑制prc2功能。 在这方面，Barnash等人利用先前开发的组合肽筛选平台轻松生成一组受JARID2-K116me3启发的拟肽EED结合剂，最终发现4-聚体微摩尔PRC2变构 ...

2022年11月11日 · EZH1β functions in skeletal muscle to block the assembly of EED, SUZ12, and EZH1α in the nucleus by binding to EED target genes in the cytoplasm, thereby controlling PRC2-EZH1 activity in...

2021年8月15日 · GSK126 and EI1 are selective and potent SAM-competitive EZH2 inhibitors, exhibiting 150-fold and 90-fold selectivity for EZH2 over EZH1, respectively, 25,47 while UNC1999, the first dual EZH2/1 inhibitor, is approximately 10-fold less potent for EZH1 than for EZH2. 48 CPI-1205 (ref. 49) and PF-06821497 (ref. 50) are already in the clinical trial...

2008年11月21日 · We have identified EZH1, a homolog of EZH2 that is physically present in a noncanonical PRC2 complex, as an H3K27 methyltransferase in vivo and in vitro. EZH1 colocalizes with the H3K27me3 mark on chromatin and preferentially preserves this mark on development-related genes in Ezh2−/− ESCs.

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 ...

2013年8月25日 · We found that our lead SAH-EZH2 peptide directly bound EED, dissociated EZH1–EED and EZH2–EED complexes and reduced the H3K27 methyltransferase activity of the PRC2 complex.

2024年12月25日 · EZH1 (Enhancer Of Zeste 1 Polycomb Repressive Complex 2 Subunit) is a Protein Coding gene. Diseases associated with EZH1 include Autism Spectrum Disorder and Weaver Syndrome. Among its related pathways are PKMTs methylate histone lysines and Interactome of polycomb repressive complex 2 (PRC2).

2020年1月16日 · We have discovered a highly potent and selective EED-targeted PROTAC that can inhibit PRC2 activity. The PROTACs target EED and its associated proteins including EZH2 and SUZ12 for elimination via the ubiquitin proteasome pathway.