Journal of labelled compounds & radiopharmaceuticals最新文献

{"title":"Towards Optimal Automated ⁶⁸Ga-Radiolabeling Conditions of the DOTA-Bisphosphonate BPAMD Without Pre-Purification of the Generator Eluate.","authors":"Céleste Souche, Juliette Fouillet, Léa Rubira, Charlotte Donzé, Audrey Sallé, Yann Dromard, Emmanuel Deshayes, Cyril Fersing","doi":"10.1002/jlcr.4128","DOIUrl":"https://doi.org/10.1002/jlcr.4128","url":null,"abstract":"<p><p>DOTA-functionalized bisphosphonates can be useful tools for PET imaging of bone metastases when radiolabeled with ⁶⁸Ga. Moreover, the versatility of DOTA allows the complexation of radiometals with therapeutic applications (e.g., ¹⁷⁷Lu), positioning these bisphosphonates as attractive theranostic agents. Among these molecules, BPAMD is a compound whose radiolabeling with ⁶⁸Ga has already been described, but only through manual methods. Thus, a fully automated protocol for ⁶⁸Ga radiolabeling of BPAMD on the GAIA® ± LUNA® synthesis module was designed, and a thorough study of the radiolabeling conditions was undertaken. [⁶⁸Ga]Ga-BPAMD was produced in good radiochemical purity (> 93%) and high radiochemical yield (> 91%) using 0.3 M HEPES buffer. The nature of the reaction vessel showed no significant effect on the radiolabeling outcome. Similarly, addition of an antiradiolysis compound to the reaction medium did not significantly improve the already excellent stability of [⁶⁸Ga]Ga-BPAMD over time. The radiolabeled product obtained by automated synthesis was evaluated in vivo in healthy mice and confirmed high accumulation in the joints and along the backbone.</p>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":" ","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142681983","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":"Simplified Flow Photosynthesis of Deuterium-Labeled Pyocyanin.","authors":"Torben Lund, Niels Jacob Krake, Poul Erik Hansen, Fatima AlZahraa Alatraktchi","doi":"10.1002/jlcr.4127","DOIUrl":"10.1002/jlcr.4127","url":null,"abstract":"<p><p>Deuterium-labeled pyocyanin was prepared from deuterium-labeled phenazine methosulfate in gram scale by a simplified flow photosynthesis in water. The main product was the protonated red form of pyocyanin-d₃ (Pyo-d₃-H⁺) in 85 % yield. Quantum chemical calculations of NMR support that nitrogen-10 is protonated. The by-products of the photolysis and the stability of the photolysis mixture were carefully characterized by LC-MS and NMR. Four by-products were identified: An isomer of pyocyanin-d₃ (9%), 8-hydroxypyocyanin-d₃ (4%), 1-hydroxyphenazine (0.4%), and phenazine (1%). The Pyo-d₃-H⁺ product was stable in the photolysis solution after storage at 8°C for 2.5 years. Pure blue pyocyanin-d₃ powder was isolated from the red photolysis solution by the Surrey method in 94 % yield. The addition of the red photolysis solution of Pyo-d₃-H⁺ (100 μM) and commercial pyocyanin (100 μM) to Pseudomonas aeruginosa cultures showed the same growth curves demonstrating that the minor impurities in the photolysis solution do not affect the growth behavior of the bacteria. The protonated deuterium-labeled pyocyanin may be used directly in biological experiments, which make the methodology extremely simple and useful for biologists.</p>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":" ","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-11-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142622142","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":"A Brief Review of Radiolabelling Nucleic Acid-Based Molecules for Tracking and Monitoring","authors":"Martin R. Edelmann,&nbsp;Filippo Sladojevich,&nbsp;Stephen M. Husbands,&nbsp;Michael B. Otteneder,&nbsp;Ian S. Blagbrough","doi":"10.1002/jlcr.4126","DOIUrl":"10.1002/jlcr.4126","url":null,"abstract":"<p>The rise of nucleic acid-based therapeutics continues apace. At the same time, the need for radiolabelled oligonucleotides for determination of spatial distribution is increasing. Complex molecular structures with mostly multiple charges and low solubility in organic solvents increase the challenge of integrating radionuclides. In preclinical research, it is important to understand the fate of new drug candidates in biodistribution studies, target binding or biotransformation studies. Depending on a specific question, the selection of a respective radiolabelling strategy is crucial. Radiometals for molecular imaging with positron emission tomography or single-photon computed tomography generally require an attached chelating agent for stable complexation of the metal with the oligonucleotide, whereas labelling using carbon-11/-14 or tritium allows incorporation of the radioisotope into the native structure without altering it. Moreover, the suitability of direct radiolabelling of the oligonucleotide of interest or indirect radiolabelling, for example, by a two-step pretargeting approach, for the study design requires consideration. This review focuses on the challenges of radiolabelling nucleic acid-based molecules with beta-plus, gamma and beta-minus emitters and their use for tracking and monitoring.</p>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 12-13","pages":"410-424"},"PeriodicalIF":0.9,"publicationDate":"2024-11-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4126","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142622239","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":"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}