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Mar 28, 2011
 |  BioCentury  |  Product Development

Epigenetic edge

Eisai, GSK back Epizyme's epigenetic discovery platform for blood, other cancers

Epizyme Inc. has been banking on the idea that potential partners will see the success of HDAC inhibitors as a good reason to place early bets on the company's histone methyltransferase drug discovery platform. Two recent deals with Eisai Co. Ltd. and GlaxoSmithKline plc say Epizyme has guessed right.

Eisai is buying into first-in-class compounds that inhibit enhancer of zeste homolog 2 (EZH2), an enzyme genetically linked to lymphoma, while GSK is collaborating with Epizyme to target an undisclosed set of histone methyltransferases (HMTs).

Like HDACs and DNA methyltransferases, HMTs regulate the expression of large gene sets by modifying the epigenetic state of chromatin. Widespread epigenetic changes occur in many cancers, but while HDAC and DNA methyltransferase inhibitors are marketed to treat specific hematological malignancies, there are no HMT inhibitors in the clinic.

According to Epizyme President and CEO Robert Gould, this is because comprehensive knowledge of HMT biochemistry is lacking....

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