Inhibitors of human EZH2 and methods of use thereof
US8895245B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Sep 12, 2011 |
| Grant date | Nov 25, 2014 |
| Priority date | — |
| Expiry date | Nov 1, 2031 |
Classification
- Technology area (CPC G)Physics
- CPC primaryG01N2333/91011
- WIPO fieldMeasurement
- WIPO sectorInstruments
Abstract
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.