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2014 Fiscal Year Final Research Report

Systematic structure optimization of the EGF receptor-inhibiting peptide through use of a screening technology

Research Project

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Project/Area Number 24590134
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Drug development chemistry
Research InstitutionThe University of Tokyo

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)

Co-Investigator(Renkei-kenkyūsha) AKAJI Kenichi  京都薬科大学, 薬学部, 教授 (60142296)
Research Collaborator MIZUGUCHI Takaaki  東京医科歯科大学, 生体材料工学研究所, 助教 (30732557)
Project Period (FY) 2012-04-01 – 2015-03-31
KeywordsEGF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
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.

Free Research Field

分子認識化学

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Published: 2016-06-03  

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