2023 Fiscal Year Annual Research Report
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 Institution | Tokyo Institute of Technology |
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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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| Keywords | Prodrug / Sialyltransferase / Acrolein |
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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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