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Possible utility of peptide-transporter-targeting [19F]dipeptides for visualization of the biodistribution of cancers by nuclear magnetic resonance imaging
https://repo.qst.go.jp/records/80590
https://repo.qst.go.jp/records/80590a48b6a9e-66fa-45e6-8c86-c78c0cc857d1
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2020-09-30 | |||||
| タイトル | ||||||
| タイトル | Possible utility of peptide-transporter-targeting [19F]dipeptides for visualization of the biodistribution of cancers by nuclear magnetic resonance 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 | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Arakawa, Hiroshi
× Arakawa, Hiroshi× Yamada, Hiroyuki× Arai, Kazutaka× Kawanishi, Takumi× Nitta, Nobuhiro× Shibata, Sayaka× Matsumoto, Eiko× Yano, Kentaro× Kato, Yukio× Kumamoto, Takuya× Aoki, Ichio× Ogihara, Takuo× Nobuhiro, Nitta× Sayaka, Shibata× Ichio, Aoki |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Stable-isotope-labeled probes suitable for magnetic resonance imaging (MRI) would have various potential medical applications, such as tumor imaging. Here, with the aim of developing MRI probes targeting peptide transporters, we synthesized a series of [19F]dipeptides by introducing one or two fluorine atoms or a trifluoromethyl group into the benzene ring of l-phenylalanyl-ψ[CS-N]-l-alanine (Phe-ψ-Ala), which is resistant to cleavage by peptidases. The mono- and difluoro dipeptides were efficiently transported by PEPT1 and PEPT2. Moreover, (3,5)-difluoro Phe-ψ-Ala was metabolically stable in human hepatocyte culture, and had a low distribution volume in mice. An acute toxicity study in mice revealed no apparent effect on body weight or behavior. The biodistribution and biodynamics of this compound could be clearly visualized by 19F-MRI in vivo, although specific signal enhancement was observed only in the bladder, but not in the tumor of tumor-xenografted mice. Although there was no specific signal enhancement of the tested compound at the tumor, the present study provides some challenging points regarding 19F-MRI probes for future investigation. | |||||
| 書誌情報 |
International Journal of Pharmaceutics 巻 586, p. 119575, 発行日 2020-08 |
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| 出版者 | ||||||
| 出版者 | Elsevier | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0378-5173 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1016/j.ijpharm.2020.119575 | |||||
| 関連サイト | ||||||
| 識別子タイプ | URI | |||||
| 関連識別子 | https://www.sciencedirect.com/science/article/pii/S0378517320305597?via%3Dihub#! | |||||
