Studies on the development of a new class of anticancer agents based on dimerization arm of the EGF receptor
Project/Area Number |
16K18910
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Research Category |
Grant-in-Aid for Young Scientists (B)
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Allocation Type | Multi-year Fund |
Research Field |
Drug development chemistry
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Research Institution | Kitasato University (2017) Tokyo Medical and Dental University (2016) |
Principal Investigator |
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Project Period (FY) |
2016-04-01 – 2018-03-31
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Project Status |
Completed (Fiscal Year 2017)
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Budget Amount *help |
¥4,030,000 (Direct Cost: ¥3,100,000、Indirect Cost: ¥930,000)
Fiscal Year 2017: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2016: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
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Keywords | EGFレセプター / 二量体化アーム / 環状ぺプチド / 細胞内送達分子 / 抗がん活性ペプチド / EGF受容体 / 二量体化阻害 / 環状ペプチド / 細胞内送達 / 細胞内薬物送達分子 / ドラッグデリバリー / 蛍光イメージング / フローサイトメトリー / 抗がん剤 / 中分子 / 薬学 / 創薬化学 / ケミカルバイオロジー / ペプチド / 有機化学 |
Outline of Final Research Achievements |
In many cancer cells, unregulated activation of epidermal growth factor (EGF) receptor often causes the aberrant cell growth. For this reason, this receptor is a useful medicinal target for the development of anticancer drugs. In this study, the results of structure-activity relationship studies of our inhibitory cyclic peptide 1 against the EGF receptor dimerization indicated that the tyrosine and threonine side-chains on the N- and C-terminal side of peptide 1, respectively, would be essential for the inhibitory effect on the EGF receptor dimerization. Besides, the addition of a polar amino acid or weakly charged histidine to the N-terminal of peptide 1 improved the inhibitory effect on the EGF receptor dimerization. In addition, fluorescein-labeled peptide 1 at the N-terminus and the derivative would be taken up by cells expressing high levels of EGF receptor, according to the experimental results with genetic engineering procedure.
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Report
(3 results)
Research Products
(4 results)
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[Journal Article] Effects of replacement and addition of an amino acid contained in a cyclic peptide corresponding to a β-hairpin loop sequence of human EGF receptor2017
Author(s)
Kobayashi K, Mizuguchi T, Hattori Y, Ohara N, Ninomiya R, Iida M, Ooe H, Yamazaki Y, Takata M, Tamamura H, Akaji K
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Journal Title
Journal of Peptide Science
Volume: 印刷中
Issue: 7-8
Pages: 581-586
DOI
Related Report
Peer Reviewed / Open Access
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