Epigenetic therapy leaps ahead with specific targeting of EZH2

Cancer Cell. 2012 Nov 13;22(5):569-70. doi: 10.1016/j.ccr.2012.10.016.


The Polycomb epigenetic silencing protein EZH2 is affected by gain-of-function somatic mutations in B cell lymphomas. Two recent reports describe the development of highly selective EZH2 inhibitors and reveal mutant EZH2 as playing an essential role in maintaining lymphoma proliferation. EZH2 inhibitors are thus a promising new targeted therapy for lymphoma.