Patent ID: 7563589

Claim:
A method of identifying a compound that inhibits the histone methyltransferase (HMTase) activity for lysine 27 of histone H3 (H3-K27) of a reconstituted complex comprising mammalian Embryonic Ectoderm Development (FED), Enhancer of Zeste Homolog 2 (EZH2), and Suppressor of Zeste 12 (SUZ12), wherein the reconstituted complex has H3-K27 HMTase activity, the method comprising: contacting the reconstituted complex with a histone substrate in the presence of a test compound; and detecting the level of H3-K27 methylation under conditions sufficient to provide H3-K27 methylation, wherein a reduction in H3-K27 methylation as compared with the level of H3-K27 methylation in the absence of the test compound indicates that the test compound is an inhibitor of the H3-K27 HMTase activity of the reconstituted complex.