Rational design of synthetic mid-sized agents that disrupt protein-protein interactions
| Project/Area Number |
25288076
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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 |
Bio-related chemistry
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| Research Institution | Kyoto University |
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Principal Investigator |
Ohkanda Junko 京都大学, 化学研究所, 准教授 (50233052)
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| Project Period (FY) |
2013-04-01 – 2016-03-31
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| Project Status |
Completed (Fiscal Year 2015)
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| Budget Amount *help |
¥18,200,000 (Direct Cost: ¥14,000,000、Indirect Cost: ¥4,200,000)
Fiscal Year 2015: ¥5,720,000 (Direct Cost: ¥4,400,000、Indirect Cost: ¥1,320,000)
Fiscal Year 2014: ¥5,720,000 (Direct Cost: ¥4,400,000、Indirect Cost: ¥1,320,000)
Fiscal Year 2013: ¥6,760,000 (Direct Cost: ¥5,200,000、Indirect Cost: ¥1,560,000)
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| Keywords | たんぱく質間相互作用 / 阻害剤 / 化学プローブ / 中分子 / K-Ras / フシコクシン / 14-3-3たんぱく質 / 14-3-3 / K-Rasたんぱく質 |
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| Outline of Final Research Achievements |
Protein-protein interactions (PPIs) play a central role in the signaling pathways that regulate many cellular functions including proliferation, differentiation, and cell death, and have emerged as a new potential clinical targets in the post-genome era. In this study, we aimed to develop a series of mid-sized molecules, of which the molecular size roughly ranges from 600 to 2,000, to recognize the large and flat interfaces and disrupt and detect intracellular PPIs. The cell-permeable bivalent inhibitors of K-Ras-PPIs and the natural product-based fluorescent probes that detect interactions of 14-3-3 and the phospholigands were designed and evaluated in vitro and in cells.
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Report
(4 results)
Research Products
(39 results)
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[Journal Article] RNA-directed amino acid coupling as a model reaction for primitive coded translation2014
Author(s)
Harada, K., Aoyama, S., Matsugami, A., Kumar, P.K.R., Katahira, M., Kato, N. and Ohkanda, J.
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Journal Title
ChemBioChem
Volume: 未定
Issue: 6
Pages: 794-798
DOI
Related Report
Peer Reviewed
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