2014 Fiscal Year Final Research Report
Integrated medicinal chemistry research of intractable diseases based on peptidic small molecules
| Project/Area Number |
23390029
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| Research Category |
Grant-in-Aid for Scientific Research (B)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Tokyo University of Pharmacy and Life Science |
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Principal Investigator |
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| Project Period (FY) |
2011-04-01 – 2015-03-31
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| Keywords | 薬学 / 創薬化学 / 生体分子 / ペプチド化学 / 有機化学 / 抗がん剤 / 難治性疾患 / リードスルー薬 |
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| Outline of Final Research Achievements |
Paying attention to the peptidic small molecule in which diverse pharmacological activity is expected, we performed a series of new integrated medicinal chemistry research to overcome intractable diseases such as cancer, genetic diseases and emerging infectious diseases.
Specific challenges are: (1) the design and synthesis of next-generation compounds of vascular disrupting agent (VDA) plinabulin which was developed by our group and is now in clinical trial, and the improvement of plinabulin as a prodrug that increases water-solubility and cancer tissue selectivity, (2) Development of a new chemotherapy for the treatment of nonsense-mediated genetic disease through the design and synthesis of new derivatives of natural product negamycin, which has a strong read-through activity, and (3) the design and synthesis of dipeptide type cysteine protease inhibitor for development of chemotherapy against severe acute respiratory syndrome (SARS).
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| Free Research Field |
医歯薬学
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