| Budget Amount *help |
¥17,160,000 (Direct Cost: ¥13,200,000、Indirect Cost: ¥3,960,000)
Fiscal Year 2020: ¥5,460,000 (Direct Cost: ¥4,200,000、Indirect Cost: ¥1,260,000)
Fiscal Year 2019: ¥5,720,000 (Direct Cost: ¥4,400,000、Indirect Cost: ¥1,320,000)
Fiscal Year 2018: ¥5,980,000 (Direct Cost: ¥4,600,000、Indirect Cost: ¥1,380,000)
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| Outline of Final Research Achievements |
Na+-pumping NADH-ubiquinone oxidoreductase (Na+-NQR) is an essential respiratory enzyme of many pathogenic bacteria such as Vibrio cholerae, and hence, a promising target of antibiotics. Natural product korormicin is a selective inhibitor of Na+-NQR, which binds to the N-terminal region of the Nqr-B subunit. We recently demonstrated that korormicin-resistance of Na+-NQR may be closely related to conformational changes of the N-terminal region. To elucidate the relationship between the conformational changes of the N-terminal region and the acquired resistance against korormicin, we investigated the chemical method that enables us to introduce a functional molecule probe to the N-terminal region. Based on protein-ligand affinity-driven NAS chemistry, we succeeded in pinpoint chemical modification of the N-terminal region.
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