• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

[镓 68]镓-舒血管肠肽,一种用于选择性细菌感染成像的潜在放射性示踪剂。

[Ga]Ga-Schizokinen, a Potential Radiotracer for Selective Bacterial Infection Imaging.

机构信息

Institute of Pharmaceutical Science, Faculty of Life Science and Medicine, King's College London, London SE1 9NH, United Kingdom.

School of Biomedical Engineering and Imaging Sciences, Faculty of Life Science and Medicine, King's College London, London SE1 7EH, United Kingdom.

出版信息

ACS Infect Dis. 2024 Aug 9;10(8):2615-2622. doi: 10.1021/acsinfecdis.4c00067. Epub 2024 Jul 16.

DOI:10.1021/acsinfecdis.4c00067
PMID:39012184
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11320569/
Abstract

Gallium-68-labeled siderophores as radiotracers have gained interest for the development of infection-specific imaging diagnostics. Here, we report radiolabeling, screening, and pharmacokinetics (PK) of gallium-68-labeled schizokinen ([Ga]Ga-SKN) as a new potential radiotracer for imaging bacterial infections. We radiolabeled SKN with ≥95% radiochemical purity. Our studies demonstrated its hydrophilic characteristics, neutral pH stability, and short-term stability in human serum and toward transchelation. uptake of [Ga]Ga-SKN by , , , and , but no uptake by , , or , demonstrated its specificity to bacterial species. Whole-body [Ga]Ga-SKN positron emission tomography (PET) combined with computerized tomography (CT) in healthy mice showed rapid renal excretion with no or minimal organ uptake. The subsequent biodistribution resembled this fast PK with rapid renal excretion with minimal blood retention and no major organ uptake and showed some dissociation of the tracer in the urine after 60 min postinjection. These findings warrant further evaluation of [Ga]Ga-SKN as a bacteria-specific radiotracer for infection imaging.

摘要

镓-68 标记的铁载体作为放射性示踪剂,因其可用于开发针对感染的特异性成像诊断而受到关注。在此,我们报告了新型潜在放射性示踪剂镓-68 标记的裂裥菌素 ([Ga]Ga-SKN) 的放射性标记、筛选和药代动力学 (PK)。我们以≥95%的放射化学纯度标记了 SKN。我们的研究表明其具有亲水性、中性 pH 稳定性以及在人血清中和向转铁蛋白转移方面的短期稳定性。[Ga]Ga-SKN 的摄取仅见于 、 、 、 和 ,而 、 或 则无摄取,表明其对细菌物种具有特异性。健康小鼠的全身 [Ga]Ga-SKN 正电子发射断层扫描 (PET) 与计算机断层扫描 (CT) 结合显示,其具有快速的肾脏排泄,无或仅有最小的器官摄取。随后的生物分布与这种快速 PK 相似,具有快速的肾脏排泄,血液滞留最小,没有主要器官摄取,并在注射后 60 分钟时在尿液中显示出一些示踪剂的解离。这些发现证明了 [Ga]Ga-SKN 作为一种用于感染成像的细菌特异性放射性示踪剂的进一步评估是合理的。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db06/11320569/6ecd3c1717ba/id4c00067_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db06/11320569/cdd8d5e22729/id4c00067_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db06/11320569/e7721c07f946/id4c00067_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db06/11320569/47ef7471ff9f/id4c00067_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db06/11320569/63bdf7781913/id4c00067_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db06/11320569/6ecd3c1717ba/id4c00067_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db06/11320569/cdd8d5e22729/id4c00067_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db06/11320569/e7721c07f946/id4c00067_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db06/11320569/47ef7471ff9f/id4c00067_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db06/11320569/63bdf7781913/id4c00067_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db06/11320569/6ecd3c1717ba/id4c00067_0005.jpg

相似文献

1
[Ga]Ga-Schizokinen, a Potential Radiotracer for Selective Bacterial Infection Imaging.[镓 68]镓-舒血管肠肽,一种用于选择性细菌感染成像的潜在放射性示踪剂。
ACS Infect Dis. 2024 Aug 9;10(8):2615-2622. doi: 10.1021/acsinfecdis.4c00067. Epub 2024 Jul 16.
2
Ga-labelled desferrioxamine-B for bacterial infection imaging.镓标记去铁胺用于细菌感染成像。
Eur J Nucl Med Mol Imaging. 2021 Feb;48(2):372-382. doi: 10.1007/s00259-020-04948-y. Epub 2020 Jul 30.
3
68Ga-siderophores for PET imaging of invasive pulmonary aspergillosis: proof of principle.68Ga- 铁载体用于侵袭性肺曲霉病的 PET 成像:原理验证。
J Nucl Med. 2010 Apr;51(4):639-45. doi: 10.2967/jnumed.109.072462.
4
More advantages in detecting bone and soft tissue metastases from prostate cancer using F-PSMA PET/CT.使用F-PSMA PET/CT检测前列腺癌骨和软组织转移方面有更多优势。
Hell J Nucl Med. 2019 Jan-Apr;22(1):6-9. doi: 10.1967/s002449910952. Epub 2019 Mar 7.
5
Imaging of bacterial infection: Harnessing positron emission tomography and Cherenkov luminescence imaging with UBI-derived octapeptide.细菌感染的影像学检查:利用 UBI 衍生的八肽进行正电子发射断层扫描和切伦科夫发光成像。
Drug Dev Res. 2023 Nov;84(7):1513-1521. doi: 10.1002/ddr.22103. Epub 2023 Aug 11.
6
Imaging of Pseudomonas aeruginosa infection with Ga-68 labelled pyoverdine for positron emission tomography.用 Ga-68 标记的吡咯并喹啉啉用于正电子发射断层扫描的铜绿假单胞菌感染成像。
Sci Rep. 2018 Oct 24;8(1):15698. doi: 10.1038/s41598-018-33895-w.
7
Preclinical evaluation of two 68Ga-siderophores as potential radiopharmaceuticals for Aspergillus fumigatus infection imaging.两种 68Ga-铁载体作为烟曲霉感染成像潜在放射性药物的临床前评价。
Eur J Nucl Med Mol Imaging. 2012 Jul;39(7):1175-83. doi: 10.1007/s00259-012-2110-3. Epub 2012 Apr 24.
8
Synthesis and Evaluation of Ga-68-Labeled Rhein for Early Assessment of Treatment-Induced Tumor Necrosis.镓-68 标记利鲁唑的合成与评价及其在治疗诱导肿瘤坏死早期评估中的应用。
Mol Imaging Biol. 2020 Jun;22(3):515-525. doi: 10.1007/s11307-019-01365-y.
9
Preclinical characterisation of gallium-68 labeled ferrichrome siderophore stereoisomers for PET imaging applications.用于正电子发射断层显像(PET)成像应用的镓-68标记高铁色素铁载体立体异构体的临床前表征
EJNMMI Radiopharm Chem. 2024 Mar 4;9(1):20. doi: 10.1186/s41181-024-00249-z.
10
Development of a New Folate-Derived Ga-68-Based PET Imaging Agent.新型叶酸衍生的 Ga-68 基 PET 成像剂的研制。
Mol Imaging Biol. 2017 Oct;19(5):754-761. doi: 10.1007/s11307-017-1049-y.

引用本文的文献

1
Total-body positron emission tomography imaging to accelerate radiotracer discovery pipelines.全身正电子发射断层扫描成像以加速放射性示踪剂发现流程。
Pharmacol Rev. 2025 Jul;77(4):100066. doi: 10.1016/j.pharmr.2025.100066. Epub 2025 May 15.
2
Radiotracers for in situ infection imaging: Experimental considerations for in vitro microbial uptake of gallium-68-labeled siderophores.用于原位感染成像的放射性示踪剂:体外微生物摄取镓-68 标记的铁载体的实验考虑因素。
Diagn Microbiol Infect Dis. 2024 Dec;110(4):116522. doi: 10.1016/j.diagmicrobio.2024.116522. Epub 2024 Sep 7.

本文引用的文献

1
Preclinical characterisation of gallium-68 labeled ferrichrome siderophore stereoisomers for PET imaging applications.用于正电子发射断层显像(PET)成像应用的镓-68标记高铁色素铁载体立体异构体的临床前表征
EJNMMI Radiopharm Chem. 2024 Mar 4;9(1):20. doi: 10.1186/s41181-024-00249-z.
2
Radiometal chelators for infection diagnostics.用于感染诊断的放射性金属螯合剂。
Front Nucl Med. 2023 Jan 9;2:1058388. doi: 10.3389/fnume.2022.1058388.
3
[Ga]Ga-Ornibactin for complex Infection Imaging Using Positron Emission Tomography.[镓]镓-Ornibactin 用于正电子发射断层扫描的复杂感染成像。
J Med Chem. 2023 Jun 8;66(11):7584-7593. doi: 10.1021/acs.jmedchem.3c00469. Epub 2023 May 30.
4
PET Imaging of Active Invasive Fungal Infections with d-[5-C]-Glutamine.使用d-[5-C]-谷氨酰胺对活动性侵袭性真菌感染进行正电子发射断层显像(PET)成像。
ACS Infect Dis. 2022 Aug 12;8(8):1663-1673. doi: 10.1021/acsinfecdis.2c00249. Epub 2022 Jul 22.
5
Characterization of siderophores from Escherichia coli strains through genome mining tools: an antiSMASH study.通过基因组挖掘工具对大肠杆菌菌株中的铁载体进行表征:一项antiSMASH研究。
AMB Express. 2022 Jun 15;12(1):74. doi: 10.1186/s13568-022-01421-x.
6
Cefiderocol for the Treatment of Multidrug-Resistant Gram-Negative Bacteria: A Systematic Review of Currently Available Evidence.头孢地尔治疗多重耐药革兰阴性菌:对现有证据的系统评价
Front Pharmacol. 2022 Apr 12;13:896971. doi: 10.3389/fphar.2022.896971. eCollection 2022.
7
Heterologous Expression and Biochemical Analysis Reveal a Schizokinen-Based Siderophore Pathway in (Cyanobacteria).异源表达和生化分析揭示 (蓝藻)中基于 Schizokinen 的铁载体途径。
Appl Environ Microbiol. 2022 Apr 12;88(7):e0237321. doi: 10.1128/aem.02373-21. Epub 2022 Mar 14.
8
Global burden of bacterial antimicrobial resistance in 2019: a systematic analysis.2019 年全球细菌对抗菌药物耐药性的负担:系统分析。
Lancet. 2022 Feb 12;399(10325):629-655. doi: 10.1016/S0140-6736(21)02724-0. Epub 2022 Jan 19.
9
The Siderophore Transporters Sit1 and Sit2 Are Essential for Utilization of Ferrichrome-, Ferrioxamine- and Coprogen-Type Siderophores in .铁载体转运蛋白Sit1和Sit2对于利用铁色素、铁胺素和粪生绿素型铁载体至关重要。
J Fungi (Basel). 2021 Sep 16;7(9):768. doi: 10.3390/jof7090768.
10
Desferrioxamine B-Mediated Pre-Clinical In Vivo Imaging of Infection by the Mold Fungus .去铁胺B介导的霉菌感染的临床前体内成像
J Fungi (Basel). 2021 Sep 8;7(9):734. doi: 10.3390/jof7090734.