调解人
表观遗传学
计算生物学
钥匙(锁)
药物发现
化学
生物
细胞生物学
生物信息学
遗传学
生态学
基因
作者
Qichao Bao,Anil Kumar,Daqing Wu,Jia Zhou
标识
DOI:10.1016/j.drudis.2024.103986
摘要
EED within the PRC2 complex is crucial for chromatin regulation, particularly in tumor development, such that its inhibition is a promising epigenetic therapeutic strategy. Significant advancement in PRC2 inhibitor development has been achieved with an approved EZH2 inhibitor in the market and with others in clinical trials. However, current EZH2 inhibitors are limited to specific blood cancers and encounter therapeutic resistance. EED stabilizes PRC2 and enhances its activity through unique allosteric mechanisms, thereby acting as both a scaffold protein and a recognizer of H3K27me3 making it an attractive drug target. This review provides an overview of epigenetic therapeutic strategies targeting EED, including allosteric inhibitors, PPI inhibitors, and PROTACs, together with brief discussions on the relevant challenges, opportunities, and future directions.
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