Polypharmacology based on dynamism of the target protein
| Project/Area Number |
26293025
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| Research Category |
Grant-in-Aid for Scientific Research (B)
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| Allocation Type | Partial Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | The University of Tokyo |
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Principal Investigator |
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| Co-Investigator(Renkei-kenkyūsha) |
ISHIKAWA Minoru 東京大学, 分子細胞生物学研究所, 准教授 (70526839)
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| Research Collaborator |
FUJII Shinya 東京大学, 分子細胞生物学研究所, 講師 (60389179)
YACHIDE Tomomi 東京大学, 分子細胞生物学研究所, 助教 (20401284)
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| Project Period (FY) |
2014-04-01 – 2017-03-31
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| Project Status |
Completed (Fiscal Year 2016)
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| Budget Amount *help |
¥17,810,000 (Direct Cost: ¥13,700,000、Indirect Cost: ¥4,110,000)
Fiscal Year 2016: ¥5,720,000 (Direct Cost: ¥4,400,000、Indirect Cost: ¥1,320,000)
Fiscal Year 2015: ¥5,720,000 (Direct Cost: ¥4,400,000、Indirect Cost: ¥1,320,000)
Fiscal Year 2014: ¥6,370,000 (Direct Cost: ¥4,900,000、Indirect Cost: ¥1,470,000)
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| Keywords | 多重薬理 / 核内受容体リガンド / 構造展開 / 阻害剤 / プロテインノックダウン / ハンチンチン / ブロモドメイン / ケイ素 / 生理活性物質 / 核内受容体 / マルチテンプレート / 分子設計 / 薬理シャペロン |
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| Outline of Final Research Achievements |
One of novel strategy in the drug development would be "polypharmacology" (or "shot-gun approach"). It focuses on the robust biological functions and captures the actions of drug from wide and various aspects. Therefore, it stands in contrast to the conventional one-drug-one-target approach. Polypharmacology drug candidates involve bio-active compounds with multiple targets, i.e., multiple pathological/pathophysiological proteins and/or genes, in drug design. The limited success of one-molecular targeted drug discovery nowadays and clarification of robustness of biological system prompt us to develop polypharmacological strategy-based new drugs. Also, functional multiplicity in addition to the multiplicity of the target proteins, i.e., protein-knockdown activity and/or pharmacological chaperon activity, were also pursued in this study.
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Report
(4 results)
Research Products
(45 results)
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[Journal Article] Design, synthesis and structure-activity relationship studies of novel sirtuin 2 (SIRT2) inhibitors with a benzamide skeleton.2015
Author(s)
Taki Sakai, Yotaro Matsumoto, Minoru Ishikawa, Kazuyuki Sugita, Yuichi Hashimoto, Nobuhiko Wakai, Akio Kitao, Era Morishita, Chikashi Toyoshima, Tomoatsu Hayashi, Tetsu Akiyama
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Journal Title
Bioorg Med Chem.
Volume: 23
Issue: 2
Pages: 328-339
DOI
Related Report
Peer Reviewed / Open Access
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[Journal Article] Structure-activity relationship study of non-steroidal NPC1L1 ligands identified through cell-based assay using pharmacological chaperone effect as a readout.2014
Author(s)
Karaki, F., Ohgane, K., Fukuda, H., Nakamura, M., Dodo, K., Hashimoto, Y.
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Journal Title
Bioorg. Med. Chem.
Volume: 22
Issue: 14
Pages: 3587-3609
DOI
Related Report
Peer Reviewed / Acknowledgement Compliant
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