2015 Fiscal Year Final Research Report
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 |
Section | 一般 |
Research Field |
Bio-related chemistry
|
Research Institution | Kyoto University |
Principal Investigator |
Ohkanda Junko 京都大学, 化学研究所, 准教授 (50233052)
|
Project Period (FY) |
2013-04-01 – 2016-03-31
|
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 |
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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Free Research Field |
生物有機化学
|