| Project/Area Number |
16K18910
|
|---|
| Research Category |
Grant-in-Aid for Young Scientists (B)
|
| Allocation Type | Multi-year Fund |
|---|
| Research Field |
Drug development chemistry
|
|---|
| Research Institution | Kitasato University (2017)
Tokyo Medical and Dental University (2016) |
|---|
Principal Investigator |
|
|---|
| Project Period (FY) |
2016-04-01 – 2018-03-31
|
| Project Status |
Completed (Fiscal Year 2017)
|
| 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)
|
|---|
| 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.
|
