For most scientists who are not deeply involved with cancer therapy the enhancer of zeste homolog 2 (EZH2) might not be the first target that comes to mind. However, this his-tone-lysine N-methyltransferase (the catalytic subunit of the polycomb repressive complex 2, which blocks gene expression by methylat-ing lysine 27 of histone H3), not only regulates embryonic development but is also a key factor for the self-renewal of cancer stem cells. Increased expression of EZH2 contributes to cancer aggressiveness and metastasis; for example, it epigenetically promotes prostate cancer by coordinating the silencing of proapoptotic microRNAs [i].
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