Development of the method for screening histone methyl transferase inhibitors utilizing the novel fluorescent probe.

组蛋白甲基转移酶（HMT）在生理条件下起着重要作用。HMT的选择性抑制剂有望成为有效的候选药物。本研究建立了一种廉价、简便的HMT活性评价方法，为HMT抑制剂的开发提供了参考。通过区分赖氨酸和甲基化赖氨酸的化学性质的差异，我们成功地估计了HMT催化反应产物甲基化赖氨酸的量。此外，我们还试图建立一种基于荧光反应的甲基化赖氨酸的高灵敏检测方法。

Histone methyltransferase (HMT) plays important roles in physiological conditions. Selective inhibitors of HMT are expected as potent drug candidate. In this study, we developed the inexpensive and easy method to evaluate the HMT activity, which is helpful in developing the HMT inhibitors. We succeeded in estimating the amount of methylated lysine which is the product of HMT-catalyzed reaction, by discriminating the difference of chemical property-between of lysine and of methylated lysine. Furthermore, we tried to develop the method for highly sensitive detection of methylated lysine based on the fluorescent response reflecting the chemical property of methylated lysine.