Application of gold-catalyzed hydroamination in sialic acids for the cancer-localized in vivo release of an immunotherapy drug
| Project/Area Number |
21K05302
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Review Section |
Basic Section 37020:Chemistry and chemical methodology of biomolecules-related
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| Research Institution | Tokyo Institute of Technology (2023)
Institute of Physical and Chemical Research (2021-2022) |
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Principal Investigator |
張 宗哲 東京工業大学, 物質理工学院, 特任助教 (00774853)
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| Project Period (FY) |
2021-04-01 – 2024-03-31
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| Project Status |
Completed (Fiscal Year 2023)
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| Budget Amount *help |
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2023: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2022: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2021: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
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| Keywords | Prodrug / Sialyltransferase / Acrolein / In vivo synthesis / Gold metal / Immunotherapy / Metal catalysis / Sialic acid / Glycoalbumin |
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| Outline of Research at the Start |
Cancer is the second leading cause of death globally, and is responsible for about 10 million deaths per year. The research could innovate the cancer immunotherapy to achieve efficiently cancer therapy for life extension and reduce numbers and death number.
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| Outline of Annual Research Achievements |
Inhibiting sialylation is thus a potential anticancer treatment strategy. However, targeting sialic acids is difficult because of the lack of selective delivery tools. I present a prodrug strategy for selectively releasing the global inhibitor of sialylation peracetylated 3Fax-Neu5Ac (PFN) in cancer cells using the reaction between phenyl azide and endogenous acrolein, which is overproduced in most cancer cells. The method significantly suppressed tumor growth in mice as effectively as PFN without causing kidney dysfunction, which is associated with PFN.
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Report
(3 results)
Research Products
(3 results)
