Molecular basis for drug discovery of dipeptidyl amino peptidases from Non-Fermented Gram-Negative Rods
Project/Area Number |
16K08322
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Research Category |
Grant-in-Aid for Scientific Research (C)
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Allocation Type | Multi-year Fund |
Section | 一般 |
Research Field |
Drug development chemistry
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Research Institution | Iwate Medical University |
Principal Investigator |
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Research Collaborator |
Roppongi Saori
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Project Period (FY) |
2016-04-01 – 2019-03-31
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Project Status |
Completed (Fiscal Year 2018)
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Budget Amount *help |
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2018: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2017: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2016: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
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Keywords | 抗菌薬 / NFGNR / 多剤耐性菌 / 歯周病菌 / 糖非発酵 / グラム陰性 / AMR / DPP / S46 / 多発性骨髄腫 / ジペプチジルアミノペプチダーゼ / 結晶構造解析 / SBDD / FE創薬 / 糖非発酵グラム陰性桿菌 / 酵素 / 感染症 / 蛋白質 / 構造生物 |
Outline of Final Research Achievements |
Depletion of effective antimicrobials due to antimicrobial abuse is a serious threat of worldwide health. This research may lead to the development of new antimicrobials. We developed compounds having an antibacterial effect against periodontitis bacteria(Porphyromonas gingivalis) and multidrug resistant bacteria (Stenotrophomonas maltophilia) using Structure Based Drug Design with Automated Research System for Drug Discovery.
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Academic Significance and Societal Importance of the Research Achievements |
2015年に採択されたWHOのアクションプランなどでは、MRSAなど緊急に新規抗菌薬の必要な菌種が取り上げられている。本研究対象のNFGNRであるStenotrophomonas maltophiliaやPorphyromonas gingivalisにも 既存の抗菌薬への耐性を有する菌株が出現しつつあり、MRSAなどに有効な抗菌薬との重複が見られる。これらNFGNRに対する特異的な抗菌薬開発は、単にそれらの菌を原因とする感染症の治療だけでなく、MRSAの治療に用いることのできる数少ない抗菌薬であるミノサイクリン、ST合剤およびマクロライド;系などの有効使用期間の延長にも繋がる。
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Report
(4 results)
Research Products
(55 results)
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[Presentation] Elucidation of substrate recognition mechanism of dipeptidyl aminopeptidase IV from Gram-negative bacteria2019
Author(s)
Akihiro Nakamura, Nobuyuki Honma, Saori Roppongi, Yoshiyuki Suzuki, Yosuke Shida, Yasumitsu Sakamoto, Koji Inaka, Hiroaki Tanaka, Kiyoito Kihira, Mitsugu Yamada, Izumi Yoshioka, Hiroaki Gouda, Takamasa Nonaka, Nobutada Tanaka, Wataru Ogasawara
Organizer
7th International GIGAKU conference in Nagaoka
Related Report
Int'l Joint Research
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[Presentation] Crystal structure analysis of bacterial dipeptidyl aminopeptidase IV2016
Author(s)
◯Roppongi, S., Tateoka, C., Suzuki, Y., Fujimoto, M., Morisawa, S., Iizuka, I., Kushibiki, C., Yonezawa, N., Ogasawara, W., Tanaka, N., Sakamoto, Y. and Nonaka, T.
Organizer
14th Conference of the Asian Crystallographic Association
Place of Presentation
Hanoi
Year and Date
2016-12-05
Related Report
Int'l Joint Research
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[Presentation] Crystal Structure of Bacterial Dipeptidyl Aminopeptidase IV Complexed with Peptide2016
Author(s)
Kushibiki, C., ◯Yonezawa, N., Roppongi, S., Tateoka, C., Suzuki, Y., Fujimoto, M., Morisawa, S., Iizuka, I., Ogasawara, W., Tanaka, N., Sakamoto, Y. and Nonaka, T.
Organizer
14th Conference of the Asian Crystallographic Association
Place of Presentation
Hanoi
Year and Date
2016-12-05
Related Report
Int'l Joint Research
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[Presentation] Structural Analysis of Dipeptidyl Peptidase 11 (DPP11) from Porphyromonas gingivalis2016
Author(s)
◯Sakamoto, Y., Suzuki, Y., Iizuka, I., Tateoka, C., Roppongi, S., Fujimoto, M., Inaka, K., Tanaka, H., Yamada, M., Ohta, K., Gouda, H., Nonaka, T., Ogasawara, W. and Tanaka, N.:
Organizer
14th Conference of the Asian Crystallographic Association
Place of Presentation
Hanoi
Year and Date
2016-12-05
Related Report
Int'l Joint Research
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[Presentation] Enzymatic characterization of S46 peptidase from pathogenic bacteria2016
Author(s)
◯Ito, Y., Nakamura, A., Roppongi, S., Sakurai, Y., Suzuki, Y., Hidaka, K., Tsuda, Y., Sakamoto, Y., Tanaka, N. and Ogasawara, W.
Organizer
The 5th International GIGAKU Conference in Nagaoka (IGCN2016)
Place of Presentation
Nagaoka
Year and Date
2016-10-07
Related Report
Int'l Joint Research
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[Presentation] Crystal structure of dipeptidyl amino peptidase 11 from Porphyromonas gingivalis2016
Author(s)
Sakamoto, Y., Suzuki, Y., Iizuka, I., Tateoka, C., Roppongi, S., Fujimoto, M., Inaka, K., Tanaka, H., Yamada, M., Ohta, K., Gouda, H., Nonaka, T., Ogasawara, W. and Tanaka, N.
Organizer
42nd Naito Conference on "In the Vanguard of Structural Biology
Place of Presentation
Sapporo
Year and Date
2016-10-06
Related Report
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[Presentation] Structure analysis of dipeptidyl peptidase 11 from Porphyromonas gingivalis.2016
Author(s)
Sakamoto, Y., Suzuki, Y., Iizuka, I., Tateoka, C., Roppongi, S., Fujimoto, M., Inaka, K., Tanaka, H., Yamada, M., Ohta, K., Gouda, H., Nonaka, T., Ogasawara, W. and Tanaka, N
Organizer
16th International Conference on the Crystallization of Biological Macromolecules
Place of Presentation
Prague
Year and Date
2016-07-05
Related Report
Int'l Joint Research
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[Presentation] Structure-Function Relationships of S46 peptidases from Non-Fermenting Gram-Negative Rods2016
Author(s)
Roppongi, S., Suzuki, I., Iizuka, I., Inaka, K., Tanaka, H., Yamada, M., Ohata, K., Nonaka, T., Ogasawara, W., Tanaka, N. and Sakamoto, Y.
Organizer
American Society for Microbiology
Place of Presentation
Boston
Year and Date
2016-06-17
Related Report
Int'l Joint Research
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