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堀家, 慎一 ; 柴, 和弘 ; Horike, Shinichi ; Shiba, Kazuhiro
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柴, 和弘
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柴, 和弘
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論文 |
Effendia, Nurmaya ; Ogawa, Kazuma ; Mishiro, Kenji ; Takarada, Takeshi ; Yamada, Daisuke ; Kitamura, Yoji ; Shiba, Kazuhiro ; Maeda, Takehiko ; Odani, Akira ; 小川, 数馬 ; 三代, 憲司 ; 宝田, 剛志 ; 北村, 陽二 ; 柴, 和弘 ; 小谷, 明
概要:
金沢大学新学術創成研究機構<br />Platelet-derived growth factor receptor β (PDGFRβ) is a transmembrane tyrosine kinase receptor and it
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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.<br />Embargo Period 12 months
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論文 |
Ogawa, Kazuma ; Ishizaki, Atsushi ; Takai, Kenichiro ; Kitamura, Yoji ; Makino, Akira ; Kozaka, Takashi ; Kiyono, Yasushi ; Shiba, Kazuhiro ; Odani, Akira ; 小川, 数馬 ; 北村, 陽二 ; 小阪, 孝史 ; 柴, 和弘 ; 小谷, 明
概要:
金沢大学新学術創成研究機構<br />67Ga-DOTA-(L-Asp)11 and 67Ga-DOTA-(L-Asp)14, which have been developed as bone imaging agents, showed
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a high accumulation in bone and a rapid blood clearance in mice. However, peptides composed of D-amino acids are more stable in vivo than those composed of their L-equivalents. In this study, 67Ga-DOTA-(D-Asp)n (n = 2, 5, 8, 11, or 14) were synthesized using the Fmoc-based solid-phase methodology and evaluated. In hydroxyapatite binding assay, binding of 67Ga-DOTA-(D-Asp)n tended to increase with increasing length of the amino acid chain. 67Ga-DOTA-(D-Asp)11 and 67Ga-DOTA-(D-Asp)14 caused a high accumulation of radioactivity in the bones of the mice. However, the results for 67Ga-DOTA-(D-Asp)n and 67Ga-DOTA-(L-Asp)n were comparable. In urine analyses, the proportion of intact complex after injection of 67Ga-DOTA-(D-Asp)14 was significantly higher than that of 67Ga-DOTA-(L-Asp)14. Although 67Ga-DOTA-(D-Asp)14 was more stable than 67Ga-DOTA-(L-Asp)14, the properties of 67Ga-DOTA-(D-Asp)n and 67Ga-DOTA-(L-Asp)n as bone imaging agents may be comparable. © 2017 The Author(s).
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その他 |
柴, 和弘 ; Shiba, Kazuhiro
概要:
取得学位 : 博士(医学), 学位授与番号 : 医博乙第1129号, 学位授与年月日:平成3年6月5日,学位授与年:1991
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論文 |
柴, 和弘
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[学会開催報告][Reviews]
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論文 |
柴, 和弘
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研究紹介 / Reviews
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論文 |
柴, 和弘
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論文 |
柴, 和弘
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