| Item type |
学術雑誌論文 / Journal Article(1) |
| 公開日 |
2025-02-04 |
| タイトル |
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|
タイトル |
The N-acetyltransferase 10 inhibitor [11C]remodelin: synthesis and preliminary positron emission tomography study in mice |
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言語 |
en |
| 言語 |
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|
言語 |
eng |
| 資源タイプ |
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資源タイプ識別子 |
http://purl.org/coar/resource_type/c_6501 |
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資源タイプ |
journal article |
| 著者 |
Luo Rui
Yiding Zhang
Kumata Katsushi
Xie Lin
Yusuke Kurihara
Ogawa Masanao
Tomomi Kokufuta
Nengaki Nobuki
Feng Wang
Zhang Ming-Rong
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| 抄録 |
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内容記述タイプ |
Abstract |
|
内容記述 |
Background: 4-(4-Cyanophenyl)-2-(2-cyclopentylidenehydrazinyl)thiazole (remodelin) is a potent N-acetyltransferase 10 (NAT10) inhibitor. This compound inhibits tumors and weakens tumor resistance to antitumor drugs. Moreover, remodelin has been found to enhance healthspan in an animal model of the human accelerated ageing syndrome. In this study, we synthesized C-11-labelled remodelin ([11C]remodelin) for the first time as a positron emission tomography (PET) probe and assessed its biodistribution in mice using PET.
Results: [11C]Remodelin was synthesized by the reaction of a boron ester precursor (1) with hydrogen [11C]cyanide, which was prepared from the cyclotron-produced [11C]carbon dioxide via [11C]methane. The decay-corrected radiochemical yield of [11C]remodelin was 6.2 ± 2.3 % (n = 20, based on [11C]carbon dioxide) with a synthesis time of 45 min and radiochemical purity of > 90%. A PET study with [11C]remodelin showed high uptake of radioactivity in the heart, liver, and small intestine of mice. The metabolite analysis indicated moderate metabolism of [11C]remodelin in the heart.
Conclusions: In the present study, we successfully synthesized [11C]remodelin and assessed its biodistribution of radioactivity in the mouse organs and tissues with PET. We are planning to prepare tumor and inflammatory models in which overexpression of NAT10 is possibly induced and conduct PET imaging for these animal models with [11C]remodelin to elucidate the relationship between NAT10 and diseases. |
| 書誌情報 |
EJNMMI Radiopharmacy and Chemistry
発行日 2025-02
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| 出版者 |
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出版者 |
Springer Nature |
| ISSN |
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収録物識別子タイプ |
ISSN |
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収録物識別子 |
2365-421X |
| DOI |
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識別子タイプ |
DOI |
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関連識別子 |
10.1186/s41181-025-00330-1 |
