| Item type |
学術雑誌論文 / Journal Article(1) |
| 公開日 |
2022-01-31 |
| タイトル |
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タイトル |
Development of novel radiogallium-labeled bone imaging agents using oligo-aspartic acid peptides as carriers |
| 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 |
| ID登録 |
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ID登録 |
10.24517/00065240 |
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ID登録タイプ |
JaLC |
| 著者 |
Ogawa, Kazuma
Ishizaki, Atsushi
Takai, Kenichiro
Kitamura, Yoji
Kiwada, Tatsuto
Shiba, Kazuhiro
Odani, Akira
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| 著者別表示 |
小川, 数馬
北村, 暘二
柴, 和弘
小谷, 明
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| 提供者所属 |
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内容記述タイプ |
Other |
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内容記述 |
金沢大学疾患モデル総合研究センター |
| 書誌情報 |
PLoS ONE
巻 8,
号 12,
p. e84335,
発行日 2013-12-31
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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 |
1932-6203 |
| DOI |
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関連タイプ |
isIdenticalTo |
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識別子タイプ |
DOI |
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関連識別子 |
10.1371/journal.pone.0084335 |
| 出版者 |
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出版者 |
Public Library of Science |
| 抄録 |
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内容記述タイプ |
Abstract |
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内容記述 |
68Ga (T1/2 = 68 min, a generator-produced nuclide) has great potential as a radionuclide for clinical positron emission tomography (PET). Because poly-glutamic and poly-aspartic acids have high affinity for hydroxyapatite, to develop new bone targeting 68Ga-labeled bone imaging agents for PET, we used 1,4,7,10-tetraazacyclododecane-1,4,7,10- tetraacetic acid (DOTA) as a chelating site and conjugated aspartic acid peptides of varying lengths. Subsequently, we compared Ga complexes, Ga-DOTA-(Asp)n (n = 2, 5, 8, 11, or 14) with easy-to-handle 67Ga, with the previously described 67Ga-DOTA complex conjugated bisphosphonate, 67Ga-DOTA-Bn-SCN-HBP. After synthesizing DOTA-(Asp)n by a Fmoc-based solid-phase method, complexes were formed with 67Ga, resulting in 67Ga-DOTA-(Asp)n with a radiochemical purity of over 95% after HPLC purification. In hydroxyapatite binding assays, the binding rate of 67Ga-DOTA-(Asp)n increased with the increase in the length of the conjugated aspartate peptide. Moreover, in biodistribution experiments, 67Ga-DOTA-(Asp) 8, 67Ga-DOTA-(Asp)11, and 67Ga-DOTA- (Asp)14 showed high accumulation in bone (10.5±1.5, 15.1±2.6, and 12.8±1.7% ID/g, respectively) but were barely observed in other tissues at 60 min after injection. Although bone accumulation of 67Ga-DOTA-(Asp)n was lower than that of 67Ga-DOTA-Bn-SCN-HBP, blood clearance of 67Ga-DOTA-(Asp)n was more rapid. Accordingly, the bone/blood ratios of 67Ga-DOTA-(Asp) 11 and 67Ga-DOTA-(Asp)14 were comparable with those of 67Ga-DOTA-Bn-SCN-HBP. In conclusion, these data provide useful insights into the drug design of 68Ga-PET tracers for the diagnosis of bone disorders, such as bone metastases. © 2013 Ogawa et al. |
| 内容記述 |
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内容記述タイプ |
Other |
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内容記述 |
CC-BY 4.0 |
| 権利 |
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権利情報 |
Copyright © 2013 Ogawa et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. |
| 著者版フラグ |
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出版タイプ |
VoR |
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出版タイプResource |
http://purl.org/coar/version/c_970fb48d4fbd8a85 |
| 関連URI |
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識別子タイプ |
URI |
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関連識別子 |
http://www.plosone.org/ |
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関連名称 |
http://www.plosone.org/ |
| 関連URI |
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識別子タイプ |
URI |
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関連識別子 |
https://journals.plos.org/plosone/article?id=10.1371/journal.pone.0084335 |
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関連名称 |
https://journals.plos.org/plosone/article?id=10.1371/journal.pone.0084335 |
ME-PR-SHIBA-K-8-e84335.pdf (540.0 kB)
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