KUNTZ KEVIN WAYNE,KNUTSON SARAH KATHLEEN,WIGLE TIMOTHY JAMES NELSON
申请号：
IN2135/KOLNP/2014
公开号：
IN2014KN02135A
申请日:
2014.10.09
申请国别(地区):
IN
年份:
2015
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.
