| Budget Amount *help |
¥13,390,000 (Direct Cost: ¥10,300,000、Indirect Cost: ¥3,090,000)
Fiscal Year 2009: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
Fiscal Year 2008: ¥3,770,000 (Direct Cost: ¥2,900,000、Indirect Cost: ¥870,000)
Fiscal Year 2007: ¥7,280,000 (Direct Cost: ¥5,600,000、Indirect Cost: ¥1,680,000)
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| Research Abstract |
I have tried to develop a novel method of inhibitor design of such enzymes exemplified to a neuraminidase Vibrio cholerae neuraminidase (VCNA) of which crystal structure was reported in 1994 and most potent inhibitor was reported in 1971. As a result, a potent inhibitor for Vibrio cholerae neuramnidase was developed using mechanism-based labeling information of key amino acid residues, design of a skeleton of focused library based on labeling information, screening of the focused library, and elimination of promiscuous inhibitor by detergent-based assay to afford potent (Ki=73nM) and selective inhibitor among viral, bacterial, and mammal neuraminidases.
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