Construction of Research Platform for Discovery of Covalent Drugs

2015 Fiscal Year Final Research Report

• Project/Area Number: 26620137
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Bio-related chemistry
• Research Institution: Kyushu University
• Principal Investigator: Ojida Akio 九州大学, 薬学研究科(研究院), 教授 (10343328)
• Project Period (FY): 2014-04-01 – 2016-03-31
• Keywords: タンパク質 / コバレントドラッグ / 化合物ライブラリー / スクリーニング

Outline of Final Research Achievements

Covent drug is agent that inhibits protein functions through the the formation of a specific covalent bond with a target protein. In this research, we constracted the research platform for development of new covalent drug. We found that alpha-chlorofluoroacetyl group is a mild reactive group suitable for covalent drug. Based on this finding, we prepared a compound library composed of the small molecules, which are appended with a alpha-chlorofluoroacetyl group. To apply this compound library f, we constructed the fluorescence assay system for screening a covalent drug for tuberculosis.

Free Research Field

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