SAR studies for epigenetic research based on natural product synthesis

基因表达机制的紊乱与包括癌症在内的多种疾病有关。我们一直专注于通过组蛋白选择性甲基化控制机制，支持DNA结构，作为药物发现的新靶点。在这项研究中，我们开发了一种有效的化学合成(+)- chae催生素的方法，它是一种有前途的组蛋白甲基化抑制剂之一。该方法可制备各种类似物。最后，我们已经成功地创造了一种新的有效的组蛋白甲基转移酶G9a的小分子抑制剂，这是已知的癌症疾病的原因。

The disorder of gene expression machinery is involved in various diseases including cancer. We have been focusing on controlling mechanism by selective methylation of histone protein that supports the structure of DNA as a novel target for drug discovery. In this study, we have developed an efficient method for the chemical synthesis of (+)-chaetocin, which is one of the promising inhibitors of histone methylation. This method allowed for the preparation of various analogs. Finally, we have succeeded in creating a novel and potent small molecule inhibitor of histone methyltransferase G9a, which is known to be responsible for cancerous diseases.