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F-FIMP：一种用于区分肿瘤组织和炎症的 LAT1 特异性 PET 探针。

F-FIMP: a LAT1-specific PET probe for discrimination between tumor tissue and inflammation.

机构信息

Laboratory for Pathophysiological and Health Science, RIKEN Center for Biosystems Dynamics Research and Center for Life Science Technologies, Kobe, Hyogo, 650-0047, Japan.

Novel PET Diagnostics Laboratory, RIKEN Innovation Center, Hyogo, 650-0047, Japan.

出版信息

Sci Rep. 2019 Oct 31;9(1):15718. doi: 10.1038/s41598-019-52270-x.

DOI:10.1038/s41598-019-52270-x
PMID:31673030
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6823354/
Abstract

Positron emission tomography (PET) imaging can assist in the early-phase diagnostic and therapeutic evaluation of tumors. Here, we report the radiosynthesis, small animal PET imaging, and biological evaluation of a L-type amino acid transporter 1 (LAT1)-specific PET probe, F-FIMP. This probe demonstrates increased tumor specificity, compared to existing tumor-specific PET probes (F-FET, C-MET, and F-FDG). Evaluation of probes by in vivo PET imaging, F-FIMP showed intense accumulation in LAT1-positive tumor tissues, but not in inflamed lesions, whereas intense accumulation of F-FDG was observed in both tumor tissues and in inflamed lesions. Metabolite analysis showed that F-FIMP was stable in liver microsomes, and mice tissues (plasma, urine, liver, pancreas, and tumor). Investigation of the protein incorporation of F-FIMP showed that it was not incorporated into protein. Furthermore, the expected mean absorbed dose of F-FIMP in humans was comparable or slightly higher than that of F-FDG and indicated that F-FIMP may be a safe PET probe for use in humans. F-FIMP may provide improved specificity for tumor diagnosis, compared to F-FDG, F-FET, and C-MET. This probe may be suitable for PET imaging for glioblastoma and the early-phase monitoring of cancer therapy outcomes.

摘要

正电子发射断层扫描（PET）成像可辅助肿瘤的早期诊断和治疗评估。在此，我们报告了 L 型氨基酸转运蛋白 1（LAT1）特异性 PET 探针 F-FIMP 的放射性合成、小动物 PET 成像和生物学评价。与现有的肿瘤特异性 PET 探针（F-FET、C-MET 和 F-FDG）相比，该探针显示出更高的肿瘤特异性。通过体内 PET 成像评估探针，F-FIMP 在 LAT1 阳性肿瘤组织中表现出强烈的积聚，而在炎症病变中则没有，而 F-FDG 则在肿瘤组织和炎症病变中均有强烈积聚。代谢产物分析表明，F-FIMP 在肝微粒体和小鼠组织（血浆、尿液、肝脏、胰腺和肿瘤）中稳定。对 F-FIMP 蛋白掺入的研究表明，它未掺入蛋白。此外，F-FIMP 在人体内的预期平均吸收剂量与 F-FDG 相当或略高，表明 F-FIMP 可能是一种安全的 PET 探针，可用于人体。与 F-FDG、F-FET 和 C-MET 相比，F-FIMP 可为肿瘤诊断提供更高的特异性。该探针可能适用于脑胶质瘤的 PET 成像和癌症治疗结果的早期监测。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5b2/6823354/71e4c93b65b1/41598_2019_52270_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5b2/6823354/f1665fa209ed/41598_2019_52270_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5b2/6823354/a84b3958549b/41598_2019_52270_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5b2/6823354/31a8191e3c6a/41598_2019_52270_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5b2/6823354/2b00ebc9e2e7/41598_2019_52270_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5b2/6823354/151871e53a82/41598_2019_52270_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5b2/6823354/cdca554328c4/41598_2019_52270_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5b2/6823354/71e4c93b65b1/41598_2019_52270_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5b2/6823354/f1665fa209ed/41598_2019_52270_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5b2/6823354/a84b3958549b/41598_2019_52270_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5b2/6823354/31a8191e3c6a/41598_2019_52270_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5b2/6823354/2b00ebc9e2e7/41598_2019_52270_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5b2/6823354/151871e53a82/41598_2019_52270_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5b2/6823354/cdca554328c4/41598_2019_52270_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5b2/6823354/71e4c93b65b1/41598_2019_52270_Fig7_HTML.jpg

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本文引用的文献

1
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J Nucl Med. 2018 May;59(5):733-739. doi: 10.2967/jnumed.117.204032. Epub 2018 Mar 9.
2
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BMC Med Imaging. 2017 Dec 28;17(1):66. doi: 10.1186/s12880-017-0237-1.
3
Novel therapeutic approaches targeting L-type amino acid transporters for cancer treatment.
人诱导多能干细胞衍生的心肌细胞和畸胎瘤移植后的代谢变化
iScience. 2024 Oct 23;27(11):111234. doi: 10.1016/j.isci.2024.111234. eCollection 2024 Nov 15.
4
Synthesis and Application of a Near-Infrared Light-Emitting Fluorescent Probe for Specific Imaging of Cancer Cells with High Sensitivity and Selectivity.近红外光致发光荧光探针的合成及其对高灵敏度和选择性的癌细胞特异性成像的应用。
Drug Des Devel Ther. 2024 Jan 10;18:29-41. doi: 10.2147/DDDT.S439038. eCollection 2024.
5
CD98 heavy chain as a prognostic biomarker and target for cancer treatment.CD98重链作为癌症治疗的预后生物标志物和靶点。
Front Oncol. 2023 Sep 26;13:1251100. doi: 10.3389/fonc.2023.1251100. eCollection 2023.
6
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4
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Korean J Radiol. 2016 May-Jun;17(3):424-34. doi: 10.3348/kjr.2016.17.3.424. Epub 2016 Apr 14.
5
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6
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7
Transport of 3-fluoro-L-α-methyl-tyrosine by tumor-upregulated L-type amino acid transporter 1: a cause of the tumor uptake in PET.肿瘤上调的 L 型氨基酸转运蛋白 1 对 3-氟-L-α-甲基酪氨酸的转运：导致 PET 肿瘤摄取的原因。
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8
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Clin Radiol. 2011 Apr;66(4):366-82. doi: 10.1016/j.crad.2010.12.004. Epub 2011 Jan 26.
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Cell. 2010 Apr 2;141(1):39-51. doi: 10.1016/j.cell.2010.03.014.