发明名称 |
INHIBITORS OF HUMAN EZH2, AND METHODS OF USE THEREOF |
摘要 |
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. |
申请公布号 |
EP2825161(A1) |
申请公布日期 |
2015.01.21 |
申请号 |
EP20130711265 |
申请日期 |
2013.03.12 |
申请人 |
EPIZYME, INC. |
发明人 |
KUNTZ, KEVIN, WAYNE;KNUTSON, SARAH, KATHLEEN;WIGLE, TIMOTHY JAMES, NELSON |
分类号 |
A61K31/00;A61K31/4162;A61K31/497;A61K31/52;A61P35/00;C12Q1/68;G01N33/50 |
主分类号 |
A61K31/00 |
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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