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    Inhibitors of Human EZH2 and Methods of Use Thereof
    3.
    发明申请
    Inhibitors of Human EZH2 and Methods of Use Thereof 有权
    人类EZH2抑制剂及其使用方法

    公开(公告)号：US20130303555A1

    公开(公告)日：2013-11-14

    申请号：US13949026

    申请日：2013-07-23

    Applicant: Epizyme, Inc.

    Inventor： Robert A. Copeland ,  Victoria M. Richon ,  Margaret D. Scott ,  Christopher J. Sneeringer ,  Kevin W. Kuntz ,  Sarah K. Knutson ,  Roy M. Pollock

    IPC: C07D493/04 ,  C12Q1/68

    CPC classification number: A61K31/7076 ,  C07D473/34 ,  C07D493/04 ,  C12Q1/48 ,  C12Q1/6876 ,  G01N33/5011 ,  G01N33/57426 ,  G01N2333/91011

    Abstract: The invention relates to determining the presence of an EZH2 gene mutation in a sample from a subject and inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono-through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.

    Abstract translation: 本发明涉及确定来自受试者的样品中EZH2基因突变的存在和抑制人组蛋白甲基转移酶EZH2的野生型和某些突变形式，其是催化单通三甲基化的PRC2复合物的催化亚单位 赖氨酸27在组蛋白H3（H3-K27）上。 在一个实施方案中，抑制对于EZH2的突变体形式是选择性的，使得与某些癌症相关的H3-K27的三甲基化被抑制。 该方法可用于治疗包括滤泡性淋巴瘤和弥漫性大B细胞淋巴瘤（DLBCL）的癌症。 还提供了用于鉴定EZH2的突变形式的小分子选择性抑制剂的方法以及用于测定受试者中对EZH2抑制剂的反应性的方法。

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