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 |
US2017065600(A1) |
申请公布日期 |
2017.03.09 |
申请号 |
US201615132610 |
申请日期 |
2016.04.19 |
申请人 |
EPIZYME, INC. |
发明人 |
Kuntz Kevin Wayne;Knutson Sarah Kathleen;Wigle Timothy James Nelson;Copeland Robert A.;Richon Victoria M.;Scott Margaret D.;Sneeringer Christopher J.;Pollock Roy M. |
分类号 |
A61K31/5377;A61K31/444;A61K31/4545;A61K31/551;G01N33/50;A61K31/4439;A61K31/4427;A61K31/496;A61K31/497;A61K31/7076;A61K31/4412 |
主分类号 |
A61K31/5377 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
Cambridge MA US |