INHIBITORS OF HUMAN EZH2, AND METHODS OF USE THEREOF

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 mu...

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Main Authors SCOTT MARGARET DAVIS, KUNTZ KEVIN WAYNE, POLLOCK ROY MACFARLANE, SNEERINGER CHRISTOPHER JOHN, COPELAND ROBERT ALLEN, RICHON VICTORIA MARIE, KNUTSON SARAH KATHLEEN
Format Patent
LanguageEnglish
Korean
Published 17.02.2014
Subjects
INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES
MEASURING
PHYSICS
TESTING
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Summary: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.
Bibliography:Application Number: KR20137009166