| Item type |
学術雑誌論文 / Journal Article(1) |
| 公開日 |
2018-01-05 |
| タイトル |
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|
タイトル |
Synthesis and evaluation of radioiodinated 1-(2-[5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl]quinolin-8-yl)piperidin-4-amine derivatives for platelet-derived growth factor receptor β (PDGFRβ) imaging |
| 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 |
10.24517/00049674 |
|
ID登録タイプ |
JaLC |
| 著者 |
Effendia, Nurmaya
Ogawa, Kazuma
Mishiro, Kenji
Takarada, Takeshi
Yamada, Daisuke
Kitamura, Yoji
Shiba, Kazuhiro
Maeda, Takehiko
Odani, Akira
|
| 著者別表示 |
小川, 数馬
三代, 憲司
宝田, 剛志
北村, 陽二
柴, 和弘
小谷, 明
|
| 提供者所属 |
|
|
内容記述タイプ |
Other |
|
内容記述 |
金沢大学新学術創成研究機構 |
| 書誌情報 |
Bioorganic and Medicinal Chemistry
巻 25,
号 20,
p. 5576-5585,
発行日 2017-10-15
|
| ISSN |
|
|
収録物識別子タイプ |
ISSN |
|
収録物識別子 |
0968-0896 |
| NCID |
|
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収録物識別子タイプ |
NCID |
|
収録物識別子 |
AA10938083 |
| DOI |
|
|
関連タイプ |
isVersionOf |
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識別子タイプ |
DOI |
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関連識別子 |
10.1016/j.bmc.2017.08.025 |
| 出版者 |
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出版者 |
Elsevier Ltd |
| 抄録 |
|
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内容記述タイプ |
Abstract |
|
内容記述 |
Platelet-derived growth factor receptor β (PDGFRβ) is a transmembrane tyrosine kinase receptor and it is upregulated in various malignant tumors. Radiolabeled PDGFRβ inhibitors can be a convenient tool for the imaging of tumors overexpressing PDGFRβ. In this study, [125I]-1-(5-iodo-2-[5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl]quinoline-8-yl)piperidin-4-amine ([125I]IIQP) and [125I]-N-3-iodobenzoyl-1-(2-[5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl]quinolin-8-yl)-piperidin-4-amine ([125I]IB-IQP) were designed and synthesized, and their potential as PDGFRβ imaging agents was evaluated. In cellular uptake experiments, [125I]IIQP and [125I]IB-IQP showed higher uptake by PDGFRβ-positive cells than by PDGFRβ-negative cells, and the uptake in PDGFRβ-positive cells was inhibited by co-culture with PDGFRβ ligands. The biodistribution of both radiotracers in normal mice exhibited hepatobiliary excretion as the main route. In mice inoculated with BxPC3-luc (PDGFRβ-positive), the tumor uptake of radioactivity at 1h after the injection of [125I]IIQP was significantly higher than that after the injection of [125I]IB-IQP. These results indicated that [125I]IIQP can be a suitable PDGFRβ imaging agent. However, further modification of its structure will be required to obtain a more appropriate PDGFRβ-targeted imaging agent with a higher signal/noise ratio. © 2017. |
| 内容記述 |
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|
内容記述タイプ |
Other |
|
内容記述 |
Embargo Period 12 months |
| 権利 |
|
|
権利情報 |
Copyright © Elsevier Ltd.(CC-BY NC ND) |
| 著者版フラグ |
|
|
出版タイプ |
AM |
|
出版タイプResource |
http://purl.org/coar/version/c_ab4af688f83e57aa |
| 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.elsevier.com/locate/issn/09680896 |
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|
関連名称 |
http://www.elsevier.com/locate/issn/09680896 |
FR-PR-OGAWA-K-5576.pdf (514.7 kB)
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