Studies on the interactions between ATR and its inhibitor Gomisin N and its application to a potentiator of antitumor agents.

2015 Fiscal Year Final Research Report

• Project/Area Number: 25293029
• Research Category: Grant-in-Aid for Scientific Research (B)
• Allocation Type: Partial Multi-year Fund
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: Nigata University of Phermacy and Applied Life Sciences
• Principal Investigator: Ishiguro Masaji 新潟薬科大学, 応用生物科学部, 教授 (10280687)
• Co-Investigator(Kenkyū-buntansha): NISHIDA Hiroshi 新潟薬科大学, 応用生物科学部, 教授 (60322541) ; TAKAKU Hiroaki 新潟薬科大学, 応用生物科学部, 教授 (70350717) ; TAMIYA Minoru 新潟薬科大学, 応用生物科学部, 助教 (10468960) ; YAMAZAKI Harutake 新潟薬科大学, 応用生物科学部, 助教 (20456776)
• Project Period (FY): 2013-04-01 – 2016-03-31
• Keywords: グミシンN / 五味子 / ATR / Phosphokinase / リグナン / 抗がん活性増強 / チェックポイント

Outline of Final Research Achievements

radioactive Gomisin N was prepared for examining the interaction site of Gomisin N in the binding at ATR.
A binding mode of Gomisin N at the substrate-binding site of phosphokinase domain of ATR was examined by constructing the phosphokinase domain using a few crystal structures of phosphokinase-related proteins by homology modeling. Docking study of Gomisin N at the substrate binding site of of the domain suggested a characteristic site and new Gomisin-related new liganan derivatives were designed based on the interactions.

Free Research Field

生物機能化学