| Item type |
学術雑誌論文 / Journal Article(1) |
| 公開日 |
2022-01-27 |
| タイトル |
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|
タイトル |
Development of radiogallium-labeled peptides for platelet-derived growth factor receptor β (Pdgfrβ) imaging: Influence of different linkers |
| 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 |
|
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
Mishiro, Kenji
Shiba, Kazuhiro
Kinuya, Seigo
Ogawa, Kazuma
|
| 著者別表示 |
三代, 憲司
柴, 和弘
絹谷, 清剛
小川, 数馬
|
| 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 |
Molecules
巻 26,
号 1,
p. 41,
発行日 2021
|
| 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 |
1420-3049 |
| DOI |
|
|
関連タイプ |
isIdenticalTo |
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|
識別子タイプ |
DOI |
|
|
関連識別子 |
10.3390/molecules26010041 |
| 出版者 |
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|
出版者 |
MDPI AG |
| 抄録 |
|
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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 |
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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 |
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|
出版タイプ |
VoR |
|
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.mdpi.com/journal/molecules |
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|
関連名称 |
http://www.mdpi.com/journal/molecules |
ME-PR-SHIBA-K-26.41.pdf (897.7 kB)
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