发明名称 |
METHOD FOR DETERMINING THE SUITABILITY OF INHIBITORS OF HUMAN EZH2 IN TREATMENT |
摘要 |
<p>The invention relates to 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.</p> |
申请公布号 |
EP2614369(A2) |
申请公布日期 |
2013.07.17 |
申请号 |
EP20110824247 |
申请日期 |
2011.09.12 |
申请人 |
EPIZYME, INC. |
发明人 |
COPELAND, ROBERT ALLEN;RICHON, VICTORIA MARIE;SCOTT, MARGARET DAVIS;SNEERINGER, CHRISTOPHER JOHN;KUNTZ, KEVIN WAYNE;KNUTSON, SARAH KATHLEEN;POLLOCK, ROY MACFARLANE |
分类号 |
G01N33/50;A61K38/17;A61P35/00;C07D473/34;G01N33/53;G01N33/574;G01N33/68 |
主分类号 |
G01N33/50 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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