| Project/Area Number |
24590134
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | 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 |
SAITO Kazuki 東京大学, 大学院新領域創成科学研究科, 特任准教授 (10192585)
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| Co-Investigator(Renkei-kenkyūsha) |
AKAJI Kenichi 京都薬科大学, 薬学部, 教授 (60142296)
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| Research Collaborator |
MIZUGUCHI Takaaki 東京医科歯科大学, 生体材料工学研究所, 助教 (30732557)
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| Project Period (FY) |
2012-04-01 – 2015-03-31
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| Project Status |
Completed (Fiscal Year 2014)
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| Budget Amount *help |
¥5,460,000 (Direct Cost: ¥4,200,000、Indirect Cost: ¥1,260,000)
Fiscal Year 2014: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2013: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2012: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000)
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| Keywords | EGFレセプター / 二量化阻害 / ループ構造模倣環状ペプチド / レセプター創薬 / スクリーニング / キャピラリー電気泳動 / 質量分析 / ＥＧＦレセプター / 二量化阻害ペプチド / 親和性増強 / 側鎖改変 |
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| Outline of Final Research Achievements |
To identify the residues contributing the inhibitory activity of the previously-developed cyclic peptide against the EGF receptor dimerization, various analogs of the peptide were chemically synthesized and their activities were measured. Judged by activities of the retro-inverso and alanine-substituted analogs, the Tyr-246 side-chain was revealed to be involved in the inhibitory activity. To optimize the structure of the cyclic peptide for acquiring stronger inhibitory activity, a novel high-throughput screening technology was developed, with which affinities of peptides in a mixture solution can be evaluated simultaneously.
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