| Item type |
学術雑誌論文 / Journal Article(1) |
| 公開日 |
2022-01-28 |
| タイトル |
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タイトル |
Comparison of radioiodine- or radiobromine-labeled rgd peptides between direct and indirect labeling methods |
| 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 |
10.24517/00065219 |
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ID登録タイプ |
JaLC |
| 著者 |
Ogawa, Kazuma
Takeda, Takuya
Yokokawa, Masaru
Yu, Jing
Makino, Akira
Kiyono, Yasushi
Shiba, Kazuhiro
Kinuya, Seigo
Odani, Akira
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| 著者別表示 |
小川, 数馬
柴, 和弘
絹谷, 清剛
小谷, 明
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| 提供者所属 |
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内容記述タイプ |
Other |
|
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 |
Chemical and Pharmaceutical Bulletin
巻 66,
号 6,
p. 651-659,
発行日 2018
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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 |
0009-2363 |
| 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 |
1347-5223 |
| NCID |
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収録物識別子タイプ |
NCID |
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収録物識別子 |
AA00602100 |
| 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 |
10.1248/cpb.c18-00081 |
| 出版者 |
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出版者 |
Pharmaceutical Society of Japan |
| 抄録 |
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内容記述タイプ |
Abstract |
|
内容記述 |
Radiolabeled cyclic peptides containing the (Arg-Gly-Asp) RGD sequence for use in positron emission tomography (PET) imaging, single-photon emission computed tomography (SPECT) imaging, and targeted radionuclide therapy of cancer have been reported. In this study, RGD was used as a model carrier peptide for diagnosis and therapy of cancer. To evaluate the characteristics of radiohalogen-labeled peptides, several kinds of labeled RGD peptides [125I-c(RGDyK), 77Br-c(RGDyK), [125I]SIB-c(RGDfK), [77Br]SBrB-c(RGDfK), [125I]SIB-EG2-c(RGDfK), and [77Br]SBrB-EG2-c(RGDfK)] were designed, prepared, and evaluated. In these initial studies, 77Br (t1/2=57.0h) and 125I (t1/2=59.4d) were used because of their longer half-lives. Precursor peptides were synthesized using a standard 9-fluorenylmethyloxycarbonyl (Fmoc)-based solid-phase methodology. Radiolabeled peptides were prepared by chloramine-T method or conjugation of RGD peptides with [125I]N-succinimidyl 3-iodobenzoate ([125I]SIB) or [77Br]N-succinimidyl 3-bromobenzoate ([77Br]SBrB). Measurement of the partition coefficients, integrin binding assay, and biodistribution experiments in tumor-bearing mice were performed. 125I and 77Br labeling were successfully performed using similar methods, and in vitro characteristics and biodistributions were similar between the 125I-labeled and corresponding 77Br-labeled peptides. [125I]SIB- and [77Br]SBrB-conjugated RGD peptides showed higher partition coefficients, lower tumor uptakes, and higher intestinal uptake than 125I-c(RGDyK) and 77Br-c(RGDyK). [125I]SIB-EG2-c(RGDfK) and [77Br]SBrB-EG2-c(RGDfK), which possess an ethylene glycol linker, decreased lipophilicity and uptake in intestine compared with [125I]SIB-c(RGDfK) and [77Br]SBrB-c(RGDfK), which possess no linker. However, the improvement in biodistribution of [125I]SIB-EG2-c(RGDfK) and [77Br]SBrB-EG2-c(RGDfK)] was insufficient. In conclusion, directly radiohalogenated c(RGDyK) peptides are potentially more useful for tumor imaging and therapy than indirectly radiohalogenated ones. © 2018 The Pharmaceutical Society of Japan. |
| 権利 |
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権利情報 |
Copyright © Pharmaceutical Society of Japan 日本薬学会 |
| 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 |
https://www.jstage.jst.go.jp/browse/cpb/-char/ja/ |
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関連名称 |
https://www.jstage.jst.go.jp/browse/cpb/-char/ja/ |
| 関連URI |
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識別子タイプ |
URI |
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関連識別子 |
https://www.pharm.or.jp/ |
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関連名称 |
https://www.pharm.or.jp/ |
ME-PR-SHIBA-K-66-651.pdf (569.7 kB)
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