| アイテムタイプ |
学術雑誌論文 / Journal Article(1) |
| 公開日 |
2024-11-11 |
| タイトル |
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タイトル |
The Glutaminase-1 Inhibitor [11C-carbony]BPTES: Synthesis and 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 |
Yiding Zhang
Kumata Katsushi
Xie Lin
Yusuke Kurihara
Ogawa Masanao
Tomomi Kokufuta
Nengaki Nobuki
Zhang Ming-Rong
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| 抄録 |
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内容記述タイプ |
Abstract |
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内容記述 |
Abstract: Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) is a selective inhibitor of glutaminase-1 (GLS1), consequently inhibiting glutaminolysis. BPTES is known for its potent antitumor activity and plays a significant role in senescent cell removal. In this study, we synthesized [11C-carbonyl]BPTES ([11C]BPTES) as a positron emission tomography (PET) probe for the first time and assessed its biodistribution in mice using PET. [11C]BPTES was synthesized by the reaction of an amine precursor () with [11C-carbonyl]phenylacetyl acid anhydride ([11C]2), which was prepared from [11C]CO2 and benzyl magnesium chloride, followed by in situ treatment with
isobutyl chloroformate. The decay-corrected isolated radiochemical yield of [11C]BPTES was 9.5% (based on [11C]CO2 ) during a synthesis time of 40 min. A PET study with [11C]BPTES showed high uptake levels of radioactivity in the liver, kidney, and small intestine of mice. |
| 書誌情報 |
Pharmaceuticals
巻 16,
号 7,
p. 963,
発行日 2023-07
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| 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 |
1424-8247 |
| DOI |
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識別子タイプ |
DOI |
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関連識別子 |
10.3390/ph16070963 |
