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Journal of labelled compounds & radiopharmaceuticals最新文献

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IF 0.9 4区 医学
Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-04-09
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引用次数: 0
IF 0.9 4区 医学
Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-04-09
{"title":"","authors":"","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 4-6","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148071001","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Development of a Fully Automated FASTlab 2 Process for [18F]AlF Radiolabelling of NOTA Peptide Conjugates NOTA肽偶联物[18F] af放射标记全自动FASTlab 2工艺的开发
IF 0.9 4区 医学
Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-04-09 DOI: 10.1002/jlcr.70030
Imtiaz Khan, Jon Shales, Stuart McCluskey, Graeme McRobbie, Julian Grigg
{"title":"Development of a Fully Automated FASTlab 2 Process for [18F]AlF Radiolabelling of NOTA Peptide Conjugates","authors":"Imtiaz Khan,&nbsp;Jon Shales,&nbsp;Stuart McCluskey,&nbsp;Graeme McRobbie,&nbsp;Julian Grigg","doi":"10.1002/jlcr.70030","DOIUrl":"10.1002/jlcr.70030","url":null,"abstract":"<div>\u0000 \u0000 \u0000 <section>\u0000 \u0000 <p>Aluminium[<sup>18</sup>F]fluoride ([<sup>18</sup>F]AlF) radiochemistry offers an attractive alternative to conventional radiometals for peptide and protein labelling and has been applied in several clinical radiopharmaceuticals. The method combines the broad availability of [<sup>18</sup>F]fluoride with rapid aqueous-phase labelling under mild conditions, making it well suited to biomolecules sensitive to organic solvents or elevated temperatures. To enable routine clinical translation, we developed a fully automated [<sup>18</sup>F]AlF radiolabelling process on the GE HealthCare FASTlab 2 synthesis platform using NOTA-AMBA as a model compound. Formulated [<sup>18</sup>F]AlF-NOTA-AMBA was produced with a non–decay-corrected radiochemical yield of 63.3% ± 5.0% (<i>n</i> = 3) in a total synthesis time of 20 min. The radioactive concentration at end of synthesis was 831 ± 115 MBq/mL, with a radiochemical purity of 94.1% ± 0.5%. The molar activity was 183.3 ± 20.7 GBq/μmol. No dissociation of [<sup>18</sup>F]AlF from the NOTA chelator was observed over 4 h at room temperature, confirming excellent stability. A simple, rapid and fully automated [<sup>18</sup>F]AlF labelling method has been established on FASTlab 2. High yields were achieved using low precursor amounts (95 μg, 67.5 nmol) without HPLC purification. The method is readily adaptable to GMP-compliant production of [<sup>18</sup>F]AlF-labelled biomolecules for clinical use.</p>\u0000 </section>\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 4-6","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147645659","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
IF 0.9 4区 医学
Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-04-07
{"title":"","authors":"","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 4-6","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-04-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148133173","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
IF 0.9 4区 医学
Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-04-07
{"title":"","authors":"","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 4-6","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-04-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148068798","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis of Carbon-13 and Carbon-14 Labeled BI 690517 (Vicadrostat) and Its O-Glucuronide Metabolite BI 689875 碳-13和碳-14标记BI 690517 （Vicadrostat）及其O-Glucuronide代谢物BI 689875的合成
IF 0.9 4区 医学
Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-04-07 DOI: 10.1002/jlcr.70026
Bachir Latli, Matt Hrapchak, Maxim Chevliakov, Lalith Samankumara, Saad Khattabi, Nizar Haddad
{"title":"Synthesis of Carbon-13 and Carbon-14 Labeled BI 690517 (Vicadrostat) and Its O-Glucuronide Metabolite BI 689875","authors":"Bachir Latli,&nbsp;Matt Hrapchak,&nbsp;Maxim Chevliakov,&nbsp;Lalith Samankumara,&nbsp;Saad Khattabi,&nbsp;Nizar Haddad","doi":"10.1002/jlcr.70026","DOIUrl":"10.1002/jlcr.70026","url":null,"abstract":"<div>\u0000 \u0000 <p>Vicadrostat, also known as <b>BI 690517</b> (<b>1</b>) is a novel, potent, and selective aldosterone synthase CYP11B2 inhibitor being developed in combination with empagliflozin to slow the progression of kidney damage and reduce cardiovascular events in people with chronic kidney diseases (CDK). The stable isotope labeled <b>BI 690517</b> was obtained in a 12-step synthesis starting from aniline-<sup>13</sup><i>C</i><sub>6</sub>. The product was isolated with high chemical purity and enantiomeric excess. Carbon-14 labeled <b>BI 690517</b> was prepared in one radioactive step from a chiral iodo-analog <b>BI 764437</b> and zinc cyanide-<sup>14</sup><i>C</i>. [<sup><b>14</b></sup><b>C]-1</b> was obtained with a specific activity of 55.6 mCi/mmol (2.05 GBq/mmol), chemical and radiochemical purities higher than 98%, and with enantiomeric excess higher than 99%. Vicadrostat undergoes extensive hepatic glucuronidation to form the <i>O</i>-glucuronide <b>BI 689875</b> (<b>2</b>). Both carbon-13 and carbon-14 labeled <b>BI 689875</b> were also synthesized.</p>\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 4-6","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-04-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147627937","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
IF 0.9 4区 医学
Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-04-06
{"title":"","authors":"","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 4-6","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-04-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148131763","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Radiotheranostics With Nanoparticles: Precision Targeting in Receptor-Overexpressing Tumors 纳米粒子放射治疗：受体过表达肿瘤的精确靶向。
IF 0.9 4区 医学
Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-04-06 DOI: 10.1002/jlcr.70028
Evalyne J. Cheruiyot, David M. Wanjeh, John K. Birir, Susan W. Karuga, Beatrice K. Amugune, Claudia G. Chambers, Michael R. Lewis, Charles J. Smith, Tamer M. Sakr
{"title":"Radiotheranostics With Nanoparticles: Precision Targeting in Receptor-Overexpressing Tumors","authors":"Evalyne J. Cheruiyot,&nbsp;David M. Wanjeh,&nbsp;John K. Birir,&nbsp;Susan W. Karuga,&nbsp;Beatrice K. Amugune,&nbsp;Claudia G. Chambers,&nbsp;Michael R. Lewis,&nbsp;Charles J. Smith,&nbsp;Tamer M. Sakr","doi":"10.1002/jlcr.70028","DOIUrl":"10.1002/jlcr.70028","url":null,"abstract":"<div>\u0000 \u0000 <p>Cancer remains one of the most challenging medical conditions. Nanotechnology is revolutionizing the approach to cancer management as an efficient tool for early diagnosis, therapy and monitoring. Nanoparticles (NPs) have shown promising results in advancing precision medicine by integrating diagnostic imaging and targeted therapy within a single platform, a concept of theranostics. Nanocarriers are synthesized via the use of biocompatible materials that are functionalized with specific ligands that bind to receptors that are overexpressed on the surface of cancer cells. For theranostic purposes, these NPs are loaded with suitable radioisotopes that emit gamma, positron, alpha or beta radiation for imaging and/or therapy. Despite the significant successes, most of the work is still at the preclinical stages awaiting clinical translation. In this review, a comprehensive examination of the current state of receptor-targeted radiotheranostic NPs is presented, with a focus on their design, functionalization, receptor-specific targeting, and clinical translational potential. The role of key tumor markers is highlighted in guiding NP delivery and improving precision and therapy. The exploration of these cutting-edge advancements and associated challenges will provide insights into the revolution of radiotheranostic nanomedicine and its impact on the future of precision oncology.</p>\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 4-6","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-04-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147627928","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
IF 0.9 4区 医学
Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-04-06
{"title":"","authors":"","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 4-6","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-04-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148067222","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
IF 0.9 4区 医学
Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-03-26
{"title":"","authors":"","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 4-6","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-03-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148091883","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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