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Synthesis and evaluation of a dimeric rgd peptide as a preliminary study for radiotheranostics with radiohalogens
https://doi.org/10.24517/00065232
https://doi.org/10.24517/0006523230067508-74af-44de-bae6-4d996da6538c
| 名前 / ファイル | ライセンス | アクション |
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ME-PR-SHIBA-K-26-06107.pdf (1.8 MB)
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| Item type | 学術雑誌論文 / Journal Article(1) | |||||||||||||||
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| 公開日 | 2022-01-27 | |||||||||||||||
| タイトル | ||||||||||||||||
| タイトル | Synthesis and evaluation of a dimeric rgd peptide as a preliminary study for radiotheranostics with radiohalogens | |||||||||||||||
| 言語 | ||||||||||||||||
| 言語 | eng | |||||||||||||||
| 資源タイプ | ||||||||||||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||||||||||||
| 資源タイプ | journal article | |||||||||||||||
| ID登録 | ||||||||||||||||
| ID登録 | 10.24517/00065232 | |||||||||||||||
| ID登録タイプ | JaLC | |||||||||||||||
| 著者 |
Echigo, Hiroaki
× Echigo, Hiroaki× Mishiro, Kenji× Fuchigami, Takeshi× Shiba, Kazuhiro× Kinuya, Seigo× Ogawa, Kazuma |
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| 著者別表示 |
三代, 憲司
× 三代, 憲司
× 淵上, 剛志
× 柴, 和弘
× 絹谷, 清剛
× 小川, 数馬
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| 提供者所属 | ||||||||||||||||
| 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 |
Molecules 巻 26, 号 20, p. 6107, 発行日 2021 |
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| ISSN | ||||||||||||||||
| 収録物識別子タイプ | ISSN | |||||||||||||||
| 収録物識別子 | 1420-3049 | |||||||||||||||
| DOI | ||||||||||||||||
| 関連タイプ | isIdenticalTo | |||||||||||||||
| 識別子タイプ | DOI | |||||||||||||||
| 関連識別子 | 10.3390/molecules26206107 | |||||||||||||||
| 出版者 | ||||||||||||||||
| 出版者 | MDPI | |||||||||||||||
| 抄録 | ||||||||||||||||
| 内容記述タイプ | Abstract | |||||||||||||||
| 内容記述 | We recently developed125I-and211At-labeled monomer RGD peptides using a novel radi-olabeling method. Both labeled peptides showed high accumulation in the tumor and exhibited similar biodistribution, demonstrating their usefulness for radiotheranostics. This study applied the labeling method to a dimer RGD peptide with the aim of gaining higher accumulation in tumor tissues based on improved affinity with αvβ3 integrin. We synthesized an iodine-introduced dimer RGD peptide, E[c(RGDfK)] (6), and an 125/131 I-labeled dimer RGD peptide, E[c(RGDfK)]{[125/131I]c[RGDf(4-I)K]} ([125/131I]6), and evaluated them as a preliminary step to the synthesis of an211At-labeled dimer RGD peptide. The affinity of 6 for αvβ3 integrin was higher than that of a monomer RGD peptide. In the biodistribution experiment at 4 h postinjection, the accumulation of [125I]6 (4.12 ± 0.42% ID/g) in the tumor was significantly increased compared with that of125I-labeled monomer RGD peptide (2.93 ± 0.08% ID/g). Moreover, the accumulation of [125I]6 in the tumor was greatly inhibited by co-injection of an excess RGD peptide. However, a single injection of [131I]6 (11.1 MBq) did not inhibit tumor growth in tumor-bearing mice. We expect that the labeling method for targeted alpha therapy with211At using a dimer RGD peptide could prove useful in future clinical applications. © 2021 by the authors. Licensee MDPI, Basel, Switzerland. | |||||||||||||||
| 内容記述 | ||||||||||||||||
| 内容記述タイプ | Other | |||||||||||||||
| 内容記述 | CC-BY 4.0 | |||||||||||||||
| 権利 | ||||||||||||||||
| 権利情報 | Copyright: © 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https:// creativecommons.org/licenses/by/ 4.0/). | |||||||||||||||
| 著者版フラグ | ||||||||||||||||
| 出版タイプ | VoR | |||||||||||||||
| 出版タイプResource | http://purl.org/coar/version/c_970fb48d4fbd8a85 | |||||||||||||||
| 関連URI | ||||||||||||||||
| 識別子タイプ | URI | |||||||||||||||
| 関連識別子 | http://www.mdpi.com/journal/molecules | |||||||||||||||
| 関連名称 | http://www.mdpi.com/journal/molecules | |||||||||||||||
