2017 Fiscal Year Final Research Report
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 |
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| Research Field |
Drug development chemistry
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| Research Institution | Kitasato University (2017)
Tokyo Medical and Dental University (2016) |
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Principal Investigator |
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| Project Period (FY) |
2016-04-01 – 2018-03-31
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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 |
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| 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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| Free Research Field |
創薬化学
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