COPELAND, ROBERT ALLEN,RICHON, VICTORIA MARIE,SCOTT, MARGARET DAVIS,SNEERINGER, CHRISTOPHER JOHN,KUNTZ, KEVIN WAYNE,KNUTSON, SARAH KATHLEEN,POLLOCK, ROY MACFARLANE
申请号：
EP11824247
公开号：
EP2614369A4
申请日:
2011.09.12
申请国别(地区):
EP
年份:
2014
代理人:
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.
