2012 Fiscal Year Final Research Report
Development of new antituberculous drugs based on CoMFA 3D-QSAR analysis
| Project/Area Number |
23659506
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Infectious disease medicine
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| Research Institution | Shimane University |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
SANO Chiaki 島根大学, 医学部, 准教授 (70325059)
TATANO Yutaka 島根大学, 医学部, 助教 (70432614)
KANEHIRO Yuichi 島根大学, 医学部, 助教 (60609197)
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| Project Period (FY) |
2011 – 2012
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| Keywords | 感染防御・制御 / オートファジー |
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| Research Abstract |
We explored the possibility of producing novel compounds that can target PknG protein with serine/threonine kinase activity with a modified luciferase assay. Ascreening test using the commercial library of protein kinase inhibitor including 80 chemical compounds was run, and AX20017, which is known as a specific inhibitor against PknG targeting the ATP-binding site, was used as a control inhibitor. Fourcompounds were showed a more favorable inhibition of PknG. Molecular docking analysiswas carried out. Three of the four novel compounds interacted with a central kinase domain containing the ATP-binding pocket in silico, similar to AX20017. These four novel lead-compounds are promising candidates for anti-tuberculous drugs.
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