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Anticancer approach by targeted activation of a global inhibitor of sialyltransferases with acrolein
https://tokushima-u.repo.nii.ac.jp/records/2000208
https://tokushima-u.repo.nii.ac.jp/records/2000208cd2ef639-169e-4f90-ad06-985b56727537
名前 / ファイル | ライセンス | アクション |
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Item type | 文献 / Documents(1) | |||||||||||||||||||||||||||||
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公開日 | 2024-10-22 | |||||||||||||||||||||||||||||
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アクセス権 | open access | |||||||||||||||||||||||||||||
アクセス権URI | http://purl.org/coar/access_right/c_abf2 | |||||||||||||||||||||||||||||
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資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||||||||||||||||||||||||||
資源タイプ | journal article | |||||||||||||||||||||||||||||
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関連識別子 | https://doi.org/10.1039/d4sc00969j | |||||||||||||||||||||||||||||
関連名称 | 10.1039/d4sc00969j | |||||||||||||||||||||||||||||
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出版タイプ | VoR | |||||||||||||||||||||||||||||
出版タイプResource | http://purl.org/coar/version/c_970fb48d4fbd8a85 | |||||||||||||||||||||||||||||
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タイトル | Anticancer approach by targeted activation of a global inhibitor of sialyltransferases with acrolein | |||||||||||||||||||||||||||||
著者 |
Kasahara, Takatsugu
× Kasahara, Takatsugu
× Chang, Tsung-Che
× Yoshioka, Hiromasa
× Urano, Sayaka
× Egawa, Yasuko
× Inoue, Michiko
× 田原, 強
WEKO
1446
× Morimoto, Koji
× Pradipta, Ambara R.
× Tanaka, Katsunori
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内容記述 | Cells are covered with a thick layer of sugar molecules known as glycans. Abnormal glycosylation is a hallmark of cancer, and hypersialylation increases tumor metastasis by promoting immune evasion and inducing tumor cell invasion and migration. Inhibiting sialylation is thus a potential anticancer treatment strategy. However, targeting sialic acids is difficult because of the lack of selective delivery tools. Here, we 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 prodrug significantly suppressed tumor growth in mice as effectively as PFN without causing kidney dysfunction, which is associated with PFN. The use of sialylated glycans as immune checkpoints is gaining increasing attention, and the proposed method for precisely targeting aberrant sialylation provides a novel avenue for expanding current cancer treatments. | |||||||||||||||||||||||||||||
書誌情報 |
en : Chemical Science 巻 15, 号 25, p. 9566-9573, 発行日 2024-05-24 |
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収録物識別子タイプ | EISSN | |||||||||||||||||||||||||||||
収録物識別子 | 20416539 | |||||||||||||||||||||||||||||
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出版者 | Royal Society of Chemistry | |||||||||||||||||||||||||||||
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権利情報 | This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. | |||||||||||||||||||||||||||||
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識別子 | 409686 | |||||||||||||||||||||||||||||
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言語 | eng |