| アイテムタイプ |
学術雑誌論文 / Journal Article(1) |
| 公開日 |
2025-04-04 |
| タイトル |
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タイトル |
An 211At-labeled alpha-melanocyte stimulating hormone peptide analog for targeted alpha therapy of metastatic melanoma |
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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 |
Suzuki Hiroyuki
Yamashita Saki
Tanaka Shoko
Kannaka Kento
Sasaki Ichiro
Oshima Yasuhiro
Watanabe Shigeki
Ooe Kazuhiro
Watabe Tadashi
Ishioka Noriko
Tanaka Hiroshi
Uehara Tomoya
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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 |
Purpose: Patients who develop metastatic melanoma have a very poor prognosis, and new treatments are needed to improve the response rates. Melanocortin-1 receptor (MC1R) is a promising target for radionuclide therapy of metastatic melanoma, and alpha-melanocyte stimulating hormone (α-MSH) peptide analogs show high affinities to MC1Rs. Because targeted alpha therapy (TAT) can be a desirable treatment for metastatic melanoma, this study aimed to develop an 211At-labeled α-MSH peptide analog for TAT of metastatic melanoma.
Methods: We designed an α-MSH analog labeled with 211At using neopentyl glycol scaffold via a hydrophilic linker. Preliminary studies using 125I-labeled α-MSH analogs were performed to identify suitable hydrophilic linkers. Then, [211At]NpG-GGN4c was prepared using a procedure similar to that of the 125I-labeled counterpart, [125I]NpG-GGN4b. The biodistribution profile of [211At]NpG-GGN4c in B16F10 tumor-bearing mice was compared with that of [125I]NpG-GGN4b. B16F10 tumor-bearing mice were treated with a single dose of vehicle or [211At]NpG-GGN4c (1 or 0.4 MBq).
Results: The D-Glu-D-Arg linker was identified as the optimal hydrophilic linker because of its high affinity for MC1R and good biodistribution profile, especially with low accumulation in the liver and intestine. [211At]NpG-GGN4c showed tumor accumulation comparable to that of [125I]NpG-GGN4b and maintained the tumor radioactivity retention from 1 to 3 h postinjection. [211At]NpG-GGN4c exhibited a dose-dependent inhibitory effect on B16F10 xenograft growth without apparent body weight loss.
Conclusion: [211At]NpG-GGN4c showed dose-dependent efficacy against B16F10 xenografts, suggesting that [211At]NpG-GGN4c is a promising TAT agent for treating metastatic melanoma. |
| 書誌情報 |
European journal of nuclear medicine and molecular imaging
発行日 2025-02
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| 出版者 |
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出版者 |
Springer Nature |
| PubMed番号 |
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識別子タイプ |
PMID |
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関連識別子 |
39828865 |
| DOI |
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識別子タイプ |
DOI |
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関連識別子 |
10.1007/s00259-024-07056-3 |
