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Possible utility of peptide-transporter-targeting [19F]dipeptides for visualization of the biodistribution of cancers by nuclear magnetic resonance imaging.
Arakawa, Hiroshi; Yamada, Hiroyuki; Arai, Kazutaka; Kawanishi, Takumi; Nitta, Nobuhiro; Shibata, Sayaka; Matsumoto, Eiko; Yano, Kentaro; Kato, Yukio; Kumamoto, Takuya; Aoki, Ichio; Ogihara, Takuo.
Afiliación
  • Arakawa H; Faculty of Pharmacy, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, Japan; Laboratory of Biopharmaceutics, Faculty of Pharmacy, Takasaki University of Health and Welfare, Takasaki 370-0033, Japan.
  • Yamada H; Laboratory of Biopharmaceutics, Faculty of Pharmacy, Takasaki University of Health and Welfare, Takasaki 370-0033, Japan.
  • Arai K; Institute for Quantum Life Science, National Institutes for Quantum and Radiological Science and Technology (QST), Chiba-city 263-8555, Japan; Department of Molecular Imaging and Theranostics, National Institute of Radiological Science, QST, Chiba-city 263-8555, Japan.
  • Kawanishi T; Faculty of Pharmacy, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, Japan.
  • Nitta N; Institute for Quantum Life Science, National Institutes for Quantum and Radiological Science and Technology (QST), Chiba-city 263-8555, Japan; Department of Molecular Imaging and Theranostics, National Institute of Radiological Science, QST, Chiba-city 263-8555, Japan.
  • Shibata S; Institute for Quantum Life Science, National Institutes for Quantum and Radiological Science and Technology (QST), Chiba-city 263-8555, Japan; Department of Molecular Imaging and Theranostics, National Institute of Radiological Science, QST, Chiba-city 263-8555, Japan.
  • Matsumoto E; Laboratory of Biopharmaceutics, Faculty of Pharmacy, Takasaki University of Health and Welfare, Takasaki 370-0033, Japan.
  • Yano K; Laboratory of Biopharmaceutics, Faculty of Pharmacy, Takasaki University of Health and Welfare, Takasaki 370-0033, Japan.
  • Kato Y; Faculty of Pharmacy, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, Japan.
  • Kumamoto T; Department of Synthetic Organic Chemistry, Graduate School of Biomedical and Health Sciences, Hiroshima University, Hiroshima 734-8553, Japan.
  • Aoki I; Institute for Quantum Life Science, National Institutes for Quantum and Radiological Science and Technology (QST), Chiba-city 263-8555, Japan; Department of Molecular Imaging and Theranostics, National Institute of Radiological Science, QST, Chiba-city 263-8555, Japan.
  • Ogihara T; Laboratory of Biopharmaceutics, Faculty of Pharmacy, Takasaki University of Health and Welfare, Takasaki 370-0033, Japan; Laboratory of Clinical Pharmacokinetics, Graduate School of Pharmaceutical Sciences, Takasaki University of Health and Welfare, Takasaki 370-0033, Japan. Electronic address: togi
Int J Pharm ; 586: 119575, 2020 Aug 30.
Article en En | MEDLINE | ID: mdl-32622809
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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Simportadores / Dipéptidos / Transportador de Péptidos 1 / Neoplasias Límite: Animals / Humans / Male Idioma: En Revista: Int J Pharm Año: 2020 Tipo del documento: Article País de afiliación: Japón Pais de publicación: Países Bajos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Simportadores / Dipéptidos / Transportador de Péptidos 1 / Neoplasias Límite: Animals / Humans / Male Idioma: En Revista: Int J Pharm Año: 2020 Tipo del documento: Article País de afiliación: Japón Pais de publicación: Países Bajos