Acceleration and satisfaction of epigenetic drug discovery using profiling technology

2017 Fiscal Year Final Research Report

• Project/Area Number: 16K15616
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Digestive surgery
• Research Institution: Osaka University
• Principal Investigator: KOSEKI Jyun 大阪大学, 医学系研究科, 特任助教(常勤) (20616669)
• Co-Investigator(Kenkyū-buntansha): 今野 雅允 大阪大学, 医学系研究科, 寄附講座講師 (80618207) ; 西田 尚弘 大阪大学, 医学系研究科, 助教 (50588118) ; 川本 弘一 大阪大学, 医学部附属病院, その他 (30432470)
• Co-Investigator(Renkei-kenkyūsha): ISHII Hideshi 大阪大学, 大学院医学系研究科, 特任教授 (10280736)
• Project Period (FY): 2016-04-01 – 2018-03-31
• Keywords: 癌 / エピゲノム / 創薬 / インシリコスクリーニング

Outline of Final Research Achievements

It was very difficult in the past to screen inhibitors of JARID1B, one of epigenome regulatory factor. We have made it possible using our in silico screening technologies with large-scale computer. In silico screening has been already performed to pick up the candidate compounds from five million drug like compounds. Then, we selected first lead compounds from the picked up candidate compounds with chemical assay. We have investigated the in vitro anti-cancer effects of these lead compounds, and the after, investigated the in vivo anti-cancer effects for the part of them. We succeeded in establishing a pathway to show the synthetic evolution guidelines for lead compounds based on the functional information from these experimental results. According to this procedure, it is possible to design a more efficient drug structure.

Free Research Field

創薬物理化学、量子物理化学