多梳蛋白抑制复合物2抑制剂的药物专利分析

Patent analysis of PRC2 inhibitors

多梳蛋白抑制复合物2(polycomb repressive complex 2,PRC2)具有组蛋白甲基转移酶活性,其亚基包括zeste基因增强子同源物2(enhancer of zeste homologue 2,EZH2)和胚胎外胚层发育蛋白(embryonic ectoderm development,EED),相关小分子抑制剂的研发成为了当前表观遗传学抗肿瘤策略的热点领域。本文基于PRC2专利文献披露的信息,梳理与分析了2000—2020年PRC2抑制剂的技术发展以及对代表性药物分别进行了核心专利、临床试验和同族专利情况分析,揭示了目前在研的前沿药物发展进度,旨在为科学家和科研管理决策提供科学依据和参考借鉴。

PRC2(polycomb repressive complex 2)has the activity of histone methyltransferase,the subunits of which include EZH2 and EED.The development of related small molecule inhibitors has become a hot spot of epigenetics-based anticancer therapy.An overview of development of PRC2-related small-molecule inhibitors during the period of 2000-2020 was combed and analyzed,as well as core patents,clinical trials and patent families of the representative new drugs.This review reveals the development process of new drugs,aiming to provide evidence and references for scientists and decision-making research management.