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Synthesis and evaluation of novel radioiodinated anthranilate derivatives for in vivo imaging of vascular endothelial growth factor receptor with single photon emission computed tomography
http://hdl.handle.net/10271/00003884
http://hdl.handle.net/10271/00003884b73157eb-bd58-433f-9204-8c669e0926a8
| 名前 / ファイル | ライセンス | アクション |
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ANM-34-486.pdf (1.4 MB)
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| Item type | 学術雑誌論文 / Journal Article(1) | |||||||||||||||
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| 公開日 | 2021-08-20 | |||||||||||||||
| タイトル | ||||||||||||||||
| タイトル | Synthesis and evaluation of novel radioiodinated anthranilate derivatives for in vivo imaging of vascular endothelial growth factor receptor with single photon emission computed tomography | |||||||||||||||
| 言語 | en | |||||||||||||||
| 言語 | ||||||||||||||||
| 言語 | eng | |||||||||||||||
| キーワード | ||||||||||||||||
| 主題 | Vascular endothelial growth factor | |||||||||||||||
| キーワード | ||||||||||||||||
| 主題 | single photon emission computed tomography | |||||||||||||||
| キーワード | ||||||||||||||||
| 主題 | radioiodine | |||||||||||||||
| キーワード | ||||||||||||||||
| 主題 | angiogenesis | |||||||||||||||
| キーワード | ||||||||||||||||
| 主題 | anthranilate | |||||||||||||||
| 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 | |||||||||||||||
| その他のタイトル | ||||||||||||||||
| その他のタイトル | Small probe for VEGFR SPECT | |||||||||||||||
| 著者 |
Hirata, Masahiko
× Hirata, Masahiko
× Asano, Akihiko
× Magata, Yasuhiro
× Ohmomo, Yoshiro
× Temma, Takashi
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| 書誌情報 |
Annals of Nuclear Medicine 巻 34, 号 7, p. 486-495, 発行日 2020-07 |
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| 出版者 | Springer Nature | |||||||||||||||
| 権利 | ||||||||||||||||
| 権利情報 | "This is a post-peer-review, pre-copyedit version of an article published in ""Annals of Nuclear Medicine"". The final authenticated version is available online at: https://doi.org/10.1007/s12149-020-01475-6." | |||||||||||||||
| 抄録 | ||||||||||||||||
| 内容記述タイプ | Abstract | |||||||||||||||
| 内容記述 | Objective Angiogenesis facilitates tumor survival and promotes malignancy. The vascular endothelial growth factor (VEGF)/VEGF receptor (VEGFR) tyrosine kinase (TK) signaling pathway is a key factor mediating angiogenesis, suggesting that this pathway may be a target for diagnosis and therapy. In this study, we aimed to develop small molecule radioiodinated probes applicable for in vivo VEGFR imaging considering the versatility and usefulness of single photon emission computed tomography (SPECT). Methods We designed and synthesized 4 radioiodinated anthranilate compounds (6a?d) based on the structure of an anticancer drug targeting VEGFR-TK. The inhibitory potencies of corresponding cold compounds 4a?d and in vitro stability of compounds 6a?d were assessed by cellular proliferation inhibition assays and radio thin-layer chromatography after incubation in neutral solution. In vivo biodistributions were evaluated by determining radioactivity in tissues of interest after intravenous injection of test compounds in tumor-bearing mice. In vitro and in vivo blocking experiments using a selective VEGFR-TK inhibitor and SPECT/computed tomography (CT) imaging were performed in tumor-bearing mice. Results The radioiodinated compounds 6a?d were obtained with more than 68.0% radiochemical yield and more than 95% radiochemical purity. Because compounds 4a?d showed high inhibitory potencies and compounds 6c and 6d showed high in vitro stability, 6c ([125I]m-NPAM) and 6d ([125I]p-NPAM) were further evaluated. Analysis of the in vivo biodistribution revealed a tumor to blood radioactivity ratio of greater than 4 at 24 h after [125I]p-NPAM administration. Accumulation of radioactivity in cultured tumor cells and tumor xenografts after [125I]p-NPAM administration was significantly blocked by inhibitor pretreatment. Tumors were clearly imaged at 24 h after [125I]p-NPAM injection with SPECT/CT in comparison to that in inhibitor-pretreated tumor-bearing mice. Conclusions [125I]p-NPAM may have potential applications as a lead compound for future development of a clinically usable VEGFR imaging probe for SPECT. |
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| 収録物識別子タイプ | ISSN | |||||||||||||||
| 収録物識別子 | 0914-7187 | |||||||||||||||
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| 収録物識別子タイプ | ISSN | |||||||||||||||
| 収録物識別子 | 1864-6433 | |||||||||||||||
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| 関連タイプ | isVersionOf | |||||||||||||||
| 識別子タイプ | PMID | |||||||||||||||
| 関連識別子 | 32385783 | |||||||||||||||
| 出版社DOI | ||||||||||||||||
| 関連タイプ | isVersionOf | |||||||||||||||
| 識別子タイプ | DOI | |||||||||||||||
| 関連識別子 | 10.1007/s12149-020-01475-6 | |||||||||||||||
| 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 | |||||||||||||||
