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Enhancer of zeste homolog 2 (EZH2)

In vitro and mouse studies suggest inhibiting EZH2 could help treat ataxia telangiectasia. In ataxia telangiectasia mutated (Atm)-deficient mice, intracerebellar injection of lentiviruses expressing Ezh2 small hairpin RNA decreased neuronal cell death compared with injection of lentiviruses expressing control shRNA and improved ataxic behavioral abnormalities. Next steps include testing either EZH2 inhibition in the model or a combination of drugs that depress histone methylation while enhancing acetylation.
Epizyme Inc. and Eisai Co. Ltd. have EPZ6438 (E7438), a selective inhibitor of EZH2, in Phase I/II testing to treat lymphoma and non-Hodgkin's lymphoma (NHL).
Constellation Pharmaceuticals Inc., Novartis AG and GlaxoSmithKline plc have EZH2 inhibitors in preclinical development to treat cancer.

SciBX 6(45); doi:10.1038/scibx.2013.1299
Published online Nov. 21, 2013

Findings unpatented; unavailable for licensing

Li, J. et al. Nat. Neurosci.;
published online Oct. 27, 2013;
Contact: Karl Herrup, The Hong Kong University of Science and Technology, Hong Kong, China
Contact: Jiali Li, Rutgers University, Piscataway, N.J.