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Development of radiogallium-labeled peptides for platelet-derived growth factor receptor β (Pdgfrβ) imaging: Influence of different linkers
https://doi.org/10.24517/00065233
https://doi.org/10.24517/00065233c5c94e5a-cdc0-4be9-b538-d64d52e4d209
名前 / ファイル | ライセンス | アクション |
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ME-PR-SHIBA-K-26.41.pdf (897.7 kB)
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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 | Development of radiogallium-labeled peptides for platelet-derived growth factor receptor β (Pdgfrβ) imaging: Influence of different linkers | |||||
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 | 10.24517/00065233 | |||||
ID登録タイプ | JaLC | |||||
著者 |
Effendi, Nurmaya
× Effendi, Nurmaya× Mishiro, Kenji× Shiba, Kazuhiro× Kinuya, Seigo× Ogawa, Kazuma |
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著者別表示 |
三代, 憲司
× 三代, 憲司× 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 1, p. 41, 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/molecules26010041 | |||||
出版者 | ||||||
出版者 | MDPI AG | |||||
抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | The purpose of this study is to develop peptide-based platelet-derived growth factor receptor β (PDGFRβ) imaging probes and examine the effects of several linkers, namely un-natural amino acids (D-alanine and β-alanine) and ethylene-glycol (EG), on the properties of Ga-DOTA(linker)-IPLPPPRRPFFK peptides. Seven radiotracers,67 Ga-DOTA-(linker)-IPLPPPRRPFFK peptides, were designed, synthesized, and evaluated. The stability and cell uptake in PDGFRβ positive peptide cells were evaluated in vitro. The biodistribution of [67 Ga]Ga-DOTA-EG2-IPLPPPRRPFFK ([67 Ga]27) and [67 Ga]Ga-DOTA-EG4-IPLPPPRRPFFK ([67 Ga]28), which were selected based on in vitro stability in murine plasma and cell uptake rates, were determined in BxPC3-luc-bearing nu/nu mice. Seven67 Ga-labeled peptides were successfully synthesized with high radiochemical yields (>85%) and purities (>99%). All evaluated radiotracers were stable in PBS (pH 7.4) at 37◦ C. However, only [67 Ga]27 and [67 Ga]28 remained more than 75% after incubation in murine plasma at 37◦ C for 1 h. [67 Ga]27 exhibited the highest BxPC3-luc cell uptake among the prepared radiolabeled peptides. As regards the results of the biodistribution experiments, the tumor-to-blood ratios of [67 Ga]27 and [67 Ga]28 at 1 h post-injection were 2.61 ± 0.75 and 2.05 ± 0.77, respectively. Co-injection of [67 Ga]27 and an excess amount of IPLPPPRRPFFK peptide as a blocking agent can significantly decrease this ratio. However, tumor accumulation was not considered sufficient. Therefore, further probe modification is required to assess tumor accumulation for in vivo imaging. © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This. | |||||
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: © 2020 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 |