{"title":"A novel Al18F-labelled NOTA-modified ubiquicidin 29-41 derivative as a bacterial infection PET imaging agent","authors":"Yuhao Jiang, Qianna Wang, Junhong Feng, Guangxing Yin, Peiwen Han, Qing Ruan, Junbo Zhang","doi":"10.1016/j.ejmech.2025.117482","DOIUrl":null,"url":null,"abstract":"The antimicrobial peptide ubiquicidin 29-41 (TGRAKRRMQYNRR) is a potential target for detecting bacterial infection. A novel UBI 29-41 derivative modified with 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA) on the amino side of lysine was synthesized and radiolabelled with Al<sup>18</sup>F, named [<sup>18</sup>F]AlF-NOTA-UBI 29-41. The novel PET tracer maintained good <em>in vitro</em> stability in saline at room temperature and mouse serum at 37 °C. <em>In vitro</em> bacterial binding experiments indicated that the tracer specifically bound to <em>Staphylococcus aureus</em>. A significant difference in the uptake of [<sup>18</sup>F]AlF-NOTA-UBI 29-41 between infected muscle and inflamed muscle was observed in biodistribution. A PET imaging study in bacterial infection mouse models revealed visible accumulation at the infection site, suggesting that the complex is a potential PET tracer for distinguishing bacterial infection from sterile inflammation.","PeriodicalId":314,"journal":{"name":"European Journal of Medicinal Chemistry","volume":"21 1","pages":""},"PeriodicalIF":6.0000,"publicationDate":"2025-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"European Journal of Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1016/j.ejmech.2025.117482","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
The antimicrobial peptide ubiquicidin 29-41 (TGRAKRRMQYNRR) is a potential target for detecting bacterial infection. A novel UBI 29-41 derivative modified with 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA) on the amino side of lysine was synthesized and radiolabelled with Al18F, named [18F]AlF-NOTA-UBI 29-41. The novel PET tracer maintained good in vitro stability in saline at room temperature and mouse serum at 37 °C. In vitro bacterial binding experiments indicated that the tracer specifically bound to Staphylococcus aureus. A significant difference in the uptake of [18F]AlF-NOTA-UBI 29-41 between infected muscle and inflamed muscle was observed in biodistribution. A PET imaging study in bacterial infection mouse models revealed visible accumulation at the infection site, suggesting that the complex is a potential PET tracer for distinguishing bacterial infection from sterile inflammation.
期刊介绍：
The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers.
A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.
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