Journal of labelled compounds & radiopharmaceuticals最新文献

{"title":"Next Generation of Solid Target Radionuclide Antibody Conjugates for Tumor Immuno-Therapy","authors":"Xingguo Hou,&nbsp;Xiangxing Kong,&nbsp;Yuan Yao,&nbsp;Song Liu,&nbsp;Ya'nan Ren,&nbsp;Muye Hu,&nbsp;Zilei Wang,&nbsp;Hua Zhu,&nbsp;Zhi Yang","doi":"10.1002/jlcr.4124","DOIUrl":"10.1002/jlcr.4124","url":null,"abstract":"<div>\u0000 \u0000 <p>Immune checkpoint therapy has emerged as an effective treatment option for various types of cancers. Key immune checkpoint molecules, such as cytotoxic T-lymphocyte-associated protein 4 (CTLA-4), programmed cell death protein 1 (PD-1), and lymphocyte activation gene 3 (LAG-3), have become pivotal targets in cancer immunotherapy. Antibodies designed to inhibit these molecules have demonstrated significant clinical efficacy. Nevertheless, the ability to monitor changes in the immune status of tumors and predict treatment response remains limited. Conventional methods, such as assessing lymphocytes in peripheral blood or conducting tumor biopsies, are inadequate for providing real-time, spatial information about T-cell distributions within heterogeneous tumors. Positron emission tomography (PET) using T-cell specific probes represents a promising and noninvasive approach to monitor both systemic and intratumoral immune changes during treatment. This technique holds substantial clinical significance and potential utility. In this paper, we review the applications of PET probes that target immune cells in molecular imaging.</p>\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 12-13","pages":"396-409"},"PeriodicalIF":0.9,"publicationDate":"2024-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142545940","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}

{"title":"Synthesis and Application of D- and 13C-Labelled tert-Butyl Hoechst Dye","authors":"Yulia A. Vlasenko,&nbsp;Avery J. To,&nbsp;Tess Fortier,&nbsp;Natasha M. Evans,&nbsp;Cole J. Lindsay,&nbsp;Peter J. Palermo,&nbsp;Thorsten Dieckmann,&nbsp;Graham K. Murphy","doi":"10.1002/jlcr.4123","DOIUrl":"10.1002/jlcr.4123","url":null,"abstract":"<p>Herein, the successful syntheses of D₃- and ¹³C-<i>N</i>-methyl and D₉-<i>tert-</i>butyl Hoechst dyes are presented. This includes the preparation of the labelled D₃- and ¹³C-<i>N-</i>methyl piperazines and D₉-<i>tert</i>-butylated hydroxytoluene precursors. The <i>tert-</i>butyl Hoechst dye is known to bind a specific RNA aptamer. Spectroscopic NMR studies of the labelled Hoechst dye-aptamer complexes allowed for the unambiguous assignment of chemical shifts, as well as the dynamics of the bound dye.</p>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 12-13","pages":"425-430"},"PeriodicalIF":0.9,"publicationDate":"2024-10-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4123","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142502181","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Preliminary Research of Radiolabeled Atezolizumab for the Noninvasive Evaluation of TNBC PD-L1 Expression In Vivo","authors":"Shuhua He,&nbsp;Lina Jia,&nbsp;Xiaobei Zheng,&nbsp;Yang Wang,&nbsp;Yuxia Liu,&nbsp;Lan Zhang","doi":"10.1002/jlcr.4122","DOIUrl":"10.1002/jlcr.4122","url":null,"abstract":"<div>\u0000 \u0000 <p>Programmed death-ligand 1 (PD-L1) expression is related to the efficacy and prognosis in triple-negative breast cancer. This study employed an indirect labeling method to synthesize [¹²⁵I]PI-Atezolizumab. The in vitro stability of [¹²⁵I]PI-Atezolizumab was assessed through incubation in phosphate buffered saline and fetal bovine serum, revealing sustained stability. Specific binding of [¹²⁵I]PI-Atezolizumab to MDA-MB-231 cells expressing humanized PD-L1 was assessed through in vitro incubation, yielding a <i>K</i>_d value comparable to that of Atezolizumab. This suggests that the labeling process did not compromise the affinity of the Atezolizumab to PD-L1. Subsequently, pharmacokinetic studies were conducted in normal mice and biodistribution experiments in tumor-bearing mice. A comparison of the biodistribution results between [¹²⁵I]PI-Atezolizumab and ¹²⁵I-labeled Atezolizumab indicated better in vivo stability for the former. Single photon emission computed tomography (SPECT)/CT imaging further confirmed the targeted specificity of [¹²⁵I]PI-Atezolizumab for PD-L1 in MDA-MB-231 xenografts, which were validated by immunohistochemistry staining. This research underscores the utility of [¹²⁵I]PI-Atezolizumab, prepared via indirect labeling, for monitoring PD-L1 in triple-negative breast cancer models.</p>\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 11","pages":"384-391"},"PeriodicalIF":0.9,"publicationDate":"2024-08-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142108129","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}

{"title":"Abstracts From the 29th International Isotope Society UK Meeting 17th November 2023","authors":"","doi":"10.1002/jlcr.4115","DOIUrl":"10.1002/jlcr.4115","url":null,"abstract":"&lt;p&gt;Matthew J. Fuchter&lt;sup&gt;1&lt;/sup&gt;&lt;/p&gt;&lt;p&gt;Department of Chemistry Imperial College London&lt;/p&gt;&lt;p&gt;Photoswitchable compounds, which can be reversibly switched between two isomers by light, continue to attract significant attention for a wide array of applications, from molecular motors, memory, and manipulators to solar thermal storage. Azoheteroarenes represent a relatively new but understudied type of photoswitch, where one or both of the aryl rings from the conventional azobenzene class has been replaced with a heteroaromatic ring. This talk will give an overview of our work in this area, initially focusing on our discovery of the arylazopyrazoles [1], which offer quantitative photoswitching and high thermal stability of the &lt;i&gt;Z&lt;/i&gt; isomer. It will go on to describe our elucidation of structure–property relationships for a wide array of comparable azoheteroaryl photoswitches [2, 3]. Through this, we have identified compounds with &lt;i&gt;Z&lt;/i&gt; isomer half-lives ranging from seconds to hours, to days and to years, and variable absorption characteristics, all through tuning of the heteraromatic ring.&lt;/p&gt;&lt;p&gt;Given the large tunability of their properties, the predictive nature of their performance, and the other potential functional opportunities afforded by usage of a heteroaromatic system, we believe the azoheteroaryl photoswitches to have huge potential in a wide range of optically addressable applications. This talk will particularly focus on the promise of such agents in photopharmacology: light-addressable drugs [4–6].&lt;/p&gt;&lt;p&gt;&lt;b&gt;References&lt;/b&gt;&lt;/p&gt;&lt;p&gt;1. \u0000 &lt;span&gt;C. E. Weston&lt;/span&gt;, &lt;span&gt;R. D. Richardson&lt;/span&gt;, &lt;span&gt;P. R. Haycock&lt;/span&gt;, &lt;span&gt;A. J. P. White&lt;/span&gt;, and &lt;span&gt;M. J. Fuchter&lt;/span&gt;, “ &lt;span&gt;Arylazopyrazoles: Azoheteroarene Photoswitches Offering Quantitative Isomerization and Long Thermal Half-Lives&lt;/span&gt;,”&lt;i&gt;Journal of the American Chemical Society&lt;/i&gt; &lt;span&gt;136&lt;/span&gt;, (&lt;span&gt;2014&lt;/span&gt;): &lt;span&gt;11878&lt;/span&gt;–&lt;span&gt;11881&lt;/span&gt;.&lt;/p&gt;&lt;p&gt;2. \u0000 &lt;span&gt;J. Calbo&lt;/span&gt;, &lt;span&gt;C. E. Weston&lt;/span&gt;, &lt;span&gt;A. J. P. White&lt;/span&gt;, &lt;span&gt;H. Rzepa&lt;/span&gt;, &lt;span&gt;J. Contreras-García&lt;/span&gt;, and &lt;span&gt;M. J. Fuchter&lt;/span&gt;, “ &lt;span&gt;Tuning Azoheteroarene Photoswitch Performance Through Heteroaryl Design&lt;/span&gt;,” &lt;i&gt;Journal of the American Chemical Society&lt;/i&gt; &lt;span&gt;139&lt;/span&gt;, (&lt;span&gt;2017&lt;/span&gt;): &lt;span&gt;1261&lt;/span&gt;–&lt;span&gt;1274&lt;/span&gt;.&lt;/p&gt;&lt;p&gt;3. \u0000 &lt;span&gt;A. Gonzalez&lt;/span&gt;, &lt;span&gt;M. Odaybat&lt;/span&gt;, &lt;span&gt;M. Le&lt;/span&gt;, et al., “ &lt;span&gt;Photocontrolled Energy Storage in Azobispyrazoles With Exceptionally Large Light Penetration Depths&lt;/span&gt;,” &lt;i&gt;Journal of the American Chemical Society&lt;/i&gt; &lt;span&gt;144&lt;/span&gt;, (&lt;span&gt;2022&lt;/span&gt;): &lt;span&gt;19430&lt;/span&gt;–&lt;span&gt;19436&lt;/span&gt;.&lt;/p&gt;&lt;p&gt;4. \u0000 &lt;span&gt;C. E. Weston&lt;/span&gt;, &lt;span&gt;A. Kraemer&lt;/span&gt;, &lt;span&gt;F. Colin&lt;/span&gt;, et al., “ &lt;span&gt;Toward Photopharmacological Antimicrobial Chemotherapy Using Photoswitchable Amidohydrolase Inhibitors&lt;/span&gt;,” &lt;i&gt;ACS Infectious Diseases&lt;/i&gt; &lt;span&gt;3&lt;/span&gt;, (&lt;span&gt;2017&lt;/span&gt;","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 10","pages":"349-356"},"PeriodicalIF":0.9,"publicationDate":"2024-08-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4115","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142008907","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Lead-212/Bismuth-212 In Vivo Generator Based on Ultrasmall Silver Telluride Nanoparticles","authors":"Runze Wang,&nbsp;Hubert Th. Wolterbeek,&nbsp;Antonia G. Denkova","doi":"10.1002/jlcr.4121","DOIUrl":"10.1002/jlcr.4121","url":null,"abstract":"<p>Radionuclide therapy employing alpha emitters holds great potential for personalized cancer treatment. However, certain challenges remain when designing alpha radiopharmaceuticals, including the lack of stability of used radioconjugates due to nuclear decay events. In this work, ultrasmall silver telluride nanoparticles with a core diameter of 2.1 nm were prepared and radiolabeled with lead-212 using a chelator-free method with a radiolabeling efficiency of 75%. The results from the in vitro radiochemical stability assay indicated a very high retention of bismuth-212 despite the internal conversion effects originating from the decay of ²¹²Pb. To further evaluate the potential of the nanoparticles, they were radiolabeled with indium-111, and their cell uptake and subcellular distribution were determined in 2D U87 cells, showing accumulation in the nucleus. Although not intentional, it was observed that the indium-111-radiolabeled nanoparticles induced efficient tumor cell killing, which was attributed to the Auger electrons emitted by indium-111. Combining the results obtained in this work with other favorable properties such as fast renal clearance and the possibility to attach targeting vectors on the surface of the nanoparticles, all well-known from the literature, these ultra-small silver telluride nanoparticles provide exciting opportunities for the design of theragnostic radiopharmaceuticals.</p>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 11","pages":"375-383"},"PeriodicalIF":0.9,"publicationDate":"2024-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4121","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141988122","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"68Ga Radiolabeling of NODASA-Functionalized Phage Display–Derived Peptides for Prospective Assessment as Tuberculosis-Specific PET Radiotracers","authors":"Christiaan A. Gouws,&nbsp;Tricia Naicker,&nbsp;Beatriz G. de la Torre,&nbsp;Fernando Albericio,&nbsp;Janie Duvenhage,&nbsp;Hendrik G. Kruger,&nbsp;Biljana Marjanovic-Painter,&nbsp;Sipho Mdanda,&nbsp;Jan R. Zeevaart,&nbsp;Thomas Ebenhan,&nbsp;Thavendran Govender","doi":"10.1002/jlcr.4120","DOIUrl":"10.1002/jlcr.4120","url":null,"abstract":"<p>This research presents the development of positron emission tomography (PET) radiotracers for detecting <i>Mycobacterium tuberculosis</i> (MTB) for the diagnosis and monitoring of tuberculosis. Two phage display–derived peptides with proven selective binding to MTB were identified for development into PET radiopharmaceuticals: H8 (linear peptide) and PH1 (cyclic peptide). We sought to functionalize H8/PH1 with NODASA, a bifunctional chelator that allows complexation of PET-compatible radiometals such as gallium-68. Herein, we report on the chelator functionalization, optimized radiosynthesis, and assessment of the radiopharmaceutical properties of [⁶⁸Ga]Ga-NODASA-H8 and [⁶⁸Ga]Ga-NODASA-PH1. Robust radiolabeling was achieved using the established routine method, indicating consistent production of a radiochemically pure product (RCP ≥ 99.6%). For respective [⁶⁸Ga]Ga-NODASA-H8 and [⁶⁸Ga]Ga-NODASA-PH1, relatively high levels of decay-corrected radiochemical yield (91.2% ± 2.3%, 86.7% ± 4.0%) and apparent molar activity (<i>A</i>_m, 3.9 ± 0.8 and 34.0 ± 5.3 GBq/μmol) were reliably achieved within 42 min, suitable for imaging purposes. Notably, [⁶⁸Ga]Ga-NODASA-PH1 remained stable in blood plasma for up to 2 h, while [⁶⁸Ga]Ga-NODASA-H8 degraded within 30 min. For both ⁶⁸Ga peptides, minimal whole-blood cell binding and plasma protein binding were observed, indicating a favorable pharmaceutical behavior. [⁶⁸Ga]Ga-NODASA-PH1 is a promising candidate for further in vitro/in vivo evaluation as a tuberculosis-specific infection imaging agent.</p>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 11","pages":"360-374"},"PeriodicalIF":0.9,"publicationDate":"2024-08-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4120","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141906806","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Application of Microfluidic Devices for Automated Two-Step Radiolabeling of Antibodies","authors":"Hiroki Jinda,&nbsp;Hiroyuki Watanabe,&nbsp;Kazuma Nakashima,&nbsp;Masahiro Ono","doi":"10.1002/jlcr.4119","DOIUrl":"10.1002/jlcr.4119","url":null,"abstract":"<div>\u0000 \u0000 <p>Radioimmunoconjugates (RICs) composed of tumor-targeting monoclonal antibodies and radionuclides have been developed for diagnostic and therapeutic application. A new radiolabeling method using microfluidic devices is expected to facilitate simpler and more rapid synthesis of RICs. In the microfluidic method, microfluidic chips can promote the reaction between reactants by mixing them efficiently, and pumping systems enable automated synthesis. In this study, we synthesized RICs by the pre-labeling method, in which the radiometal is coordinated to the chelator and then the radiolabeled chelator is incorporated into the antibodies, using microfluidic devices for the first time. As a result of examining the reaction parameters including the material of mixing units, reaction temperature, and flow rate, RICs with radiochemical purity (RCP) exceeding 90% were obtained. These high-purity RICs were successfully synthesized without any purification simply by pumping three solutions of a chelating agent, radiometal, and antibody into microfluidic devices. Under the same conditions, the RCP of RICs labeled by conventional methods was below 50%. These findings indicate the utility of microfluidic devices for automatic and rapid synthesis of high-quality RICs.</p>\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 10","pages":"341-348"},"PeriodicalIF":0.9,"publicationDate":"2024-08-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141897627","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}

{"title":"Synthesis and Preclinical Evaluation of [18F]AlF-NOTA-Asp2-PEG2-Folate as a Novel Folate-Receptor-Targeted Tracer for PET Imaging","authors":"Haoran Liang,&nbsp;Zihao Chen,&nbsp;Chunwei Mo,&nbsp;Ganghua Tang","doi":"10.1002/jlcr.4118","DOIUrl":"10.1002/jlcr.4118","url":null,"abstract":"<div>\u0000 \u0000 <p>Recently, the folate receptor (FR) has become an exciting target for the diagnosis of FR-positive malignancies. Nevertheless, suboptimal in vivo pharmacokinetic properties, particularly high uptake in the renal and hepatobiliary systems, are important limiting factors for the clinical translation of most FR-based radiotracers. In this study, we developed a novel ¹⁸F-labeled FR-targeted positron emission tomography (PET) tracer [¹⁸F]AlF-NOTA-Asp₂-PEG₂-Folate modified with a hydrophilic linker (−Asp₂-PEG₂) to optimize its pharmacokinetic properties and conducted a comprehensive preclinical assessment. The [¹⁸F]AlF-NOTA-Asp₂-PEG₂-Folate was manually synthesized within 30 min with a non-decay-corrected radiochemical yield of 16.3 ± 2.0% (<i>n</i> = 5). Among KB cells, [¹⁸F]AlF-NOTA-Asp₂-PEG₂-Folate exhibited high specificity and affinity for FR. PET/CT imaging and biodistribution experiments in KB tumor-bearing mice showed decent tumor uptake (1.7 ± 0.3% ID/g) and significantly decreased uptake in kidneys and liver (22.2 ± 2.1 and 0.3 ± 0.1% ID/g at 60 min p.i., respectively) of [¹⁸F]AlF-NOTA-Asp₂-PEG₂-Folate, compared to the known tracer [¹⁸F]AlF-NOTA-Folate (78.6 ± 5.1 and 5.3 ± 0.5 % ID/g at 90 min p.i., respectively). The favorable properties of [¹⁸F]AlF-NOTA-Asp₂-PEG₂-Folate, including its efficient synthesis, decent tumor uptake, relatively low renal uptake, and rapid clearance from most normal organs, portray it as a promising PET tracer for FR-positive tumors.</p>\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 10","pages":"334-340"},"PeriodicalIF":0.9,"publicationDate":"2024-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141748358","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}

{"title":"Direct Multi-Deuterium Labelling of Pirtobrutinib","authors":"Michal Kriegelstein,&nbsp;Jana Hojcsková,&nbsp;Miloš Hroch,&nbsp;Aleš Marek","doi":"10.1002/jlcr.4117","DOIUrl":"10.1002/jlcr.4117","url":null,"abstract":"<p>Herein, we demonstrate an efficient method for multi-deuterium labelling of pirtobrutinib—a Bruton's tyrosine kinase inhibitor recently approved by the FDA—using a straightforward hydrogen isotope exchange (HIE) reaction. A remarkably high level of deuterium incorporation was achieved using an excess of a Kerr-type iridium catalyst. The key factor in the significant deuterium labelling was the decision to employ a deuterium uniformly labelled solvent, chlorobenzene-<i>d</i>₅, at an elevated temperature. Virtually, no <i>d</i>₀–<i>d</i>₃ species were detected, with only traces of <i>d</i>₄–<i>d</i>₅ isotopomers (&lt; 5%) observable in the mass spectrum of pirtobrutinib-<i>d</i>₈, fulfilling requirements for stable isotope-labelled internal standard. The labelled compound—mainly consisting of isotopomers <i>d</i>₆–<i>d</i>₉ at 82.4% of the total abundance—was isolated in a high yield (73%) and purity (99%). Noteworthy, fluorine group acting as a directing group was observed for the first time. Significant incorporation of deuterium in <i>ortho</i>-positions, exceeding 87%, was observed. Interestingly, chlorinated solvent used in the HIE reactions was non-specifically deuterated yielding up to 0.42 deuterium per chlorobenzene molecule even at an exceptionally low iridium catalyst loading of 4.17 × 10^–2 mol%.</p>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 9","pages":"314-323"},"PeriodicalIF":0.9,"publicationDate":"2024-07-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4117","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141616680","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Fully Automated Cassette-Based Synthesis of 2-Deoxy-2-[18F]Fluorocellobiose Using Trasis AllInOne Module","authors":"Falguni Basuli,&nbsp;Jianfeng Shi,&nbsp;Swati Shah,&nbsp;Jianhao Lai,&nbsp;Dima A. Hammoud,&nbsp;Rolf E. Swenson","doi":"10.1002/jlcr.4116","DOIUrl":"10.1002/jlcr.4116","url":null,"abstract":"<div>\u0000 \u0000 <p>Due to the continuous rise in global incidence and severity of invasive fungal infections (IFIs), particularly among immunocompromised and immunodeficient patients, there is an urgent demand for swift and accurate fungal pathogen diagnosis. Therefore, the need for fungal-specific positron emission tomography (PET) imaging agents that can detect the infection in the early stages is increasing. Cellobiose, a disaccharide, is readily metabolized by fungal pathogens such as <i>Aspergillus</i> species. Recently, our group reported fluorine-18 labeled cellobiose, 2-deoxy-2-[¹⁸F]fluorocellobiose ([¹⁸F]FCB), for specific imaging of <i>Aspergillus</i> infection. The positive imaging findings with very low background signal on delayed imaging make this ligand a promising fungal-specific imaging ligand. Inspired by this result, the decision was made to automate the radiolabeling procedure for better reproducibility and to facilitate clinical translation. A Trasis AllInOne (Trasis AIO) automated module was used for this purpose. The reagent vials contain commercially available 2-deoxy-2-[¹⁸F]fluoroglucose ([¹⁸F]FDG), glucose-1-phosphate, and enzyme (cellobiose phosphorylase). A Sep-Pak cartridge was used to purify the tracer. The overall radiochemical yield was 50%–70% (<i>n</i> = 6, decay corrected) in 75-min synthesis time with a radiochemical purity of &gt; 98%. This is a highly reliable protocol to produce current good manufacturing practice (cGMP)–compliant [¹⁸F]FCB for clinical PET imaging.</p>\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 9","pages":"308-313"},"PeriodicalIF":0.9,"publicationDate":"2024-07-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141563548","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}