Synthetic post-translational modifications
| Project/Area Number |
17K19197
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| Research Category |
Grant-in-Aid for Challenging Research (Exploratory)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Biomolecular chemistry and related fields
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| Research Institution | Kyoto University |
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Principal Investigator |
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| Project Period (FY) |
2017-06-30 – 2019-03-31
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| Project Status |
Completed (Fiscal Year 2018)
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| Budget Amount *help |
¥6,500,000 (Direct Cost: ¥5,000,000、Indirect Cost: ¥1,500,000)
Fiscal Year 2018: ¥3,250,000 (Direct Cost: ¥2,500,000、Indirect Cost: ¥750,000)
Fiscal Year 2017: ¥3,250,000 (Direct Cost: ¥2,500,000、Indirect Cost: ¥750,000)
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| Keywords | ケミカルバイオロジー / 化合物ライブラリー |
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| Outline of Final Research Achievements |
Small-molecule probes that are covalently attached to a protein of interest often serve as tools for biological research by facilitating detection and purification of the protein and its binding partners. This project proposes a new approach to discovering covalent chemical probes that label specific proteins. To identify such probe-protein pairs in an unbiased way, we have been taking advantage of our in-house chemical library that consists of 1,657 electrophile synthetic compounds and 83 reactive natural products. The screening of the library isolated three promising molecules: two synthetic molecules and one natural product. We are currently in the process of analyzing their effects on the biological functions of the target proteins.
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| Academic Significance and Societal Importance of the Research Achievements |
多数のタンパク質に対して多数の化合物をスクリーニングし、「人工翻訳後修飾」を探索した例はこれまでになく、世界初。利用する反応性化合物ライブラリーは世界的に独自性が高い。成功すれば、これまでになかった新しい知識を生み出して、生理活性小分子化合物や創薬の研究方向を変革する潜在的可能性がある。
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Report
(3 results)
Research Products
(22 results)
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[Journal Article] Small-molecule screening yields a compound that inhibits the cancer-associated transcription factor Hes1 via the PHB2 chaperone.2018
Author(s)
Perron A, Nishikawa Y, Iwata J, Shimojo H, Takaya J, Kobayashi K, Imayoshi I, Mbenza NM, Takenoya M, Kageyama R, Kodama Y, Uesugi M.
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Journal Title
J Biol Chem.
Volume: 印刷中
Issue: 21
Pages: 8285-8294
DOI
Related Report
Peer Reviewed
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