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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
https://doi.org/10.24517/00049674
https://doi.org/10.24517/00049674eace99d5-b4b5-41c8-9e95-fb3926035822
名前 / ファイル | ライセンス | アクション |
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FR-PR-OGAWA-K-5576.pdf (514.7 kB)
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Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2018-01-05 | |||||
タイトル | ||||||
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
× Effendia, Nurmaya× Ogawa, Kazuma× Mishiro, Kenji× Takarada, Takeshi× Yamada, Daisuke× Kitamura, Yoji× Shiba, Kazuhiro× Maeda, Takehiko× Odani, Akira |
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著者別表示 |
小川, 数馬
× 小川, 数馬× 三代, 憲司× 宝田, 剛志× 北村, 陽二× 柴, 和弘× 小谷, 明 |
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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 |
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ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 0968-0896 | |||||
NCID | ||||||
収録物識別子タイプ | NCID | |||||
収録物識別子 | AA10938083 | |||||
DOI | ||||||
関連タイプ | isVersionOf | |||||
識別子タイプ | DOI | |||||
関連識別子 | 10.1016/j.bmc.2017.08.025 | |||||
出版者 | ||||||
出版者 | Elsevier Ltd | |||||
抄録 | ||||||
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 | ||||||
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 | ||||||
識別子タイプ | URI | |||||
関連識別子 | http://www.elsevier.com/locate/issn/09680896 | |||||
関連名称 | http://www.elsevier.com/locate/issn/09680896 |