SAR studies for epigenetic research based on natural product synthesis

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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.