Journal of labelled compounds & radiopharmaceuticals最新文献_第7页

Radiolabeling of Trastuzumab With Technetium-99m [99mTc] as a Radioligand for Screening Mentha pulegium on HER-2 Receptors 锝-99m [99mTc]放射标记曲妥珠单抗筛选HER-2受体上的脑膜炎

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-01-01 DOI: 10.1002/jlcr.70006

Narges Aryanpour, Golrokh Farnam, Farshad H. Shirazi, Soraya Shahhosseini

{"title":"Radiolabeling of Trastuzumab With Technetium-99m [99mTc] as a Radioligand for Screening Mentha pulegium on HER-2 Receptors","authors":"Narges Aryanpour, Golrokh Farnam, Farshad H. Shirazi, Soraya Shahhosseini","doi":"10.1002/jlcr.70006","DOIUrl":"10.1002/jlcr.70006","url":null,"abstract":"<div>\u0000 \u0000 The use of medicinal plants as anti-cancer agents has attracted the attention of researchers. A method is needed for screening the anti-cancer effects on HER-2 receptors. In this study, a simple method based on radioligand binding studies was developed for primary screening of medicinal plants on HER-2 receptors in vitro. Trastuzumab was conjugated to HYNIC in a chemical reaction using NHS-HYNIC. HYNIC-Trastuzumab was radiolabeled with [99mTc] using SnCl2 as a reducing agent and tricine as a coligand. Biological activities of [99mTc]Tc-HYNIC-Trastuzumab were determined in saturation binding studies using the SKBR3 cell line. The IC50 of Mentha pulegium was determined in competition with [99mTc]Tc-HYNIC-Trastuzumab on the SKBR3 cell line. Radiochemical purity was ≥ 90% ± 2.08%. Based on the results, radiolabeled Trastuzumab maintained its biological activity after labeling (immunoreactivity = 83%, Kd = 7.049 ± 1.861 nM). The IC50 of Mentha pulegium was 31.3 ± 1.3 μg/mL. [99mTc]Tc-HYNIC-Trastuzumab can be used as a radioligand in competition binding studies for primary screening of medicinal plants, peptides, and small molecules in vitro on HER-2 receptors.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145887273","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}

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Antibody Drug Conjugate Formation Using 2-14C-Iminothiolane: A Radiochemical Analysis of Sequential Lysine Conjugation, Uncloaking of a Phantom Drug-to-Antibody Ratio, and Stability of the ADC 利用2- 14c -亚氨基硫烷形成抗体药物偶联物：序列赖氨酸偶联物的放射化学分析，揭示幻药-抗体比，以及ADC的稳定性。

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-12-14 DOI: 10.1002/jlcr.70002

Michael Wallace, Michael J. Smith, John Brailsford, Difei Qiu, Alban J. Allentoff, Annie Tam, Selin Aytar, Michael Hay, Sharon Gong, Samuel Bonacorsi Jr.

{"title":"Antibody Drug Conjugate Formation Using 2-14C-Iminothiolane: A Radiochemical Analysis of Sequential Lysine Conjugation, Uncloaking of a Phantom Drug-to-Antibody Ratio, and Stability of the ADC","authors":"Michael Wallace, Michael J. Smith, John Brailsford, Difei Qiu, Alban J. Allentoff, Annie Tam, Selin Aytar, Michael Hay, Sharon Gong, Samuel Bonacorsi Jr.","doi":"10.1002/jlcr.70002","DOIUrl":"10.1002/jlcr.70002","url":null,"abstract":"<div>\u0000 \u0000 [14C]2-Iminothiolane ([14C]2-IT) served as a highly informative analytical tool to determine the rate of lysine thiolation and total addition of 2-IT to a monoclonal antibody. Specific activity measurements on [14C]2-IT modified mAbs found that lysine thiolation with 2-IT is linear regarding time and dependent on buffer strength. Conjugation with a fluorescent maleimide directly linked the free thiol-to-antibody ratio (FTAR) to the [14C]2-IT-to-antibody ratio ([14C]ITAR), providing accurate predictive information on the true number of sites proficient for payload conjugation and, by comparison with conjugation with the cytotoxic payload, quantified the absorbance from the nonconjugated cyclized N-substituted 2-iminothiolane adduct that created “phantom” drug-to-antibody ratios (PhDAR). Hydrolytic loss of the nonconjugated cyclized N-substituted 2-iminothiolane adduct was investigated using carbon-14 based radioquantitative HPLC, mass spectral analysis, and orthogonal [14C]ITAR and DAR measurements of the isolated [14C]mAb. These measurements combined to demonstrate that significant amounts of the cyclized products were shed from the [14C]ADC as [14C]thiobutyrolactone.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 14","pages":""},"PeriodicalIF":0.9,"publicationDate":"2025-12-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145756744","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

Assessment of Stability Extrapolation for Carbon-14 Labelled Compounds for the Determination of Extended Retest Periods 碳14标记化合物稳定性外推法测定延长复测周期的评价。

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-12-14 DOI: 10.1002/jlcr.70000

Antonio Moreno-Herrera, Ryan A. Bragg, Charles S. Elmore

引用次数: 0

Radiolabeled Aptamers for Bioimaging Applications in Oncology and Infectious Diseases 放射标记适体在肿瘤学和传染病生物成像中的应用。

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-12-10 DOI: 10.1002/jlcr.70001

Najeeb Ullah, Tracy Ann Bruce-Tagoe, George Adu Asamoah, Shokoufeh Soleimani, Michael K. Danquah

{"title":"Radiolabeled Aptamers for Bioimaging Applications in Oncology and Infectious Diseases","authors":"Najeeb Ullah, Tracy Ann Bruce-Tagoe, George Adu Asamoah, Shokoufeh Soleimani, Michael K. Danquah","doi":"10.1002/jlcr.70001","DOIUrl":"10.1002/jlcr.70001","url":null,"abstract":"<div>\u0000 \u0000 Radiolabeled aptamers are promising molecular probes for bioimaging because of their potential for high specificity, stability, and rapid clearance from nontarget tissues. They are single-stranded oligonucleotides labeled with radionuclides such as technetium-99m (99ᵐTc), fluorine-18 (18F), and gallium-68 (68Ga) to enable precise imaging via single-photon emission computed tomography (SPECT) and positron emission tomography (PET). The versatility of radiolabeling strategies can provide opportunities to enhance biostability and pharmacokinetics while improving imaging sensitivity. In cancer theranostics, radiolabeled aptamers can allow early detection and treatment as well as facilitate effective monitoring of therapeutic responses. The applications of radiolabeled aptamers extend to infectious disease imaging, enabling real-time tracking of infections. Despite these advances, challenges such as rapid renal clearance, immunogenicity, and the need for clinical validation persist, catalyzing further research focused on enhancing the stability of radiolabeled aptamers, improving radiolabeling efficacy, and optimizing biodistribution. Emerging strategies, including nanoparticle conjugation and hybrid bioimaging, offer a great perspective for advancing the field. This article highlights recent advancements in radiolabeled aptamers in terms of their development, bioimaging applications, and research directions to address their limitations.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 14","pages":""},"PeriodicalIF":0.9,"publicationDate":"2025-12-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145723985","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}

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Abstracts From the 30th International Isotope Society UK Meeting 15th November 2024 第30届国际同位素学会英国会议摘要，2024年11月15日

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-11-26 DOI: 10.1002/jlcr.4165

引用次数: 0

Synthesis and Characterization of 2-Thiophenemethanamine-2H5 Hydrochloride 2-噻吩甲烷胺- 2h5盐酸盐的合成与表征

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-11-21 DOI: 10.1002/jlcr.4170

Sean David William Greenwood, Pete Deardorff, William Sherman, Desmond Slade

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RETRACTED: Enhanced Control of Bacterial Wilt Disease in Tomato Plant via Transport and Penetration Tracking by Aid of 99mTc-Labeled Ralstonia solanacearum–Specific Bacteriophage 利用99mtc标记的番茄枯萎病特异性噬菌体的运输和渗透跟踪加强番茄青枯病的防治

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-11-11 DOI: 10.1002/jlcr.4169

Mohammed H. Abdel-Aal, Yasmeen A. Hasanien, Nahed A. Younis, Gamal El Didamony, Ahmed Askora, Gamal Abdelaziz

{"title":"RETRACTED: Enhanced Control of Bacterial Wilt Disease in Tomato Plant via Transport and Penetration Tracking by Aid of 99mTc-Labeled Ralstonia solanacearum–Specific Bacteriophage","authors":"Mohammed H. Abdel-Aal, Yasmeen A. Hasanien, Nahed A. Younis, Gamal El Didamony, Ahmed Askora, Gamal Abdelaziz","doi":"10.1002/jlcr.4169","DOIUrl":"10.1002/jlcr.4169","url":null,"abstract":"<div>\u0000 \u0000 In order to reduce the development of antibiotic and chemical resistance in bacterial phytopathogens like Ralstonia solanacearum, which causes bacterial wilt disease, bacteriophages are a safe and efficient biocontrol method. This research will explore how to use radioisotopes to track the bacteriophage absorption by plants from roots to leaves as a means for improving phage persistence and thereby the control of bacterial wilt disease caused by R. solanacearum. We have investigated the uptake and delivery of R. solanacearum–specific bacteriophages in tomato plants. Transferring phage through roots to leaves showed a gradual increase over time until reaching the maximal at 120 min, where the percentage of bacteriophage reaches 21.95% of the total amount of the injected radiation dose, which is considered a good sign for the ability of bacteriophage to reach the leaves and infect the pathogen through its transport system if injected directly into soil. Demonstrating in-plant translocation of R. solanacearum–specific bacteriophages and their effect of reducing bacterial wilt symptoms may significantly contribute to a better control of R. solanacearum and promote further investigations on the penetration and translocation of phages into plants.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 13","pages":""},"PeriodicalIF":0.9,"publicationDate":"2025-11-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145488751","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}

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Synthesis of BI 1584142 and BI 1810631 (Zongertinib), Two Potent HER2 Inhibitors, Labeled With Carbon-14 and With Deuterium 两种高效HER2抑制剂BI 1584142和BI 1810631 （Zongertinib）的合成，碳-14和氘标记

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-10-26 DOI: 10.1002/jlcr.4168

Bachir Latli, Eugene Chong

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Synthesis and Preclinical Evaluation of 99ᵐTc-HYNIC–Finasteride: A Novel SPECT Radiotracer Targeting 5α-Reductase in Prostate Cancer 99 - tc - hynici -非那雄胺：一种靶向前列腺癌5α-还原酶的新型SPECT示踪剂的合成及临床前评价

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-10-07 DOI: 10.1002/jlcr.4167

Saba Shirin, Syed Qaiser Shah, Ralph Santos-Oliveira, Derya Ilem-Ozdemir

{"title":"Synthesis and Preclinical Evaluation of 99ᵐTc-HYNIC–Finasteride: A Novel SPECT Radiotracer Targeting 5α-Reductase in Prostate Cancer","authors":"Saba Shirin, Syed Qaiser Shah, Ralph Santos-Oliveira, Derya Ilem-Ozdemir","doi":"10.1002/jlcr.4167","DOIUrl":"10.1002/jlcr.4167","url":null,"abstract":"<div>\u0000 \u0000 We describe the synthesis and preclinical assessment of a novel technetium-99m-labeled 5α-reductase (5AR) inhibitor, a 5AR-targeting drug, a target enzyme of prostate cancer (PCa) pathology, as a SPECT imaging probe. Finasteride was attached to 6-hydrazinonicotinic acid (HYNIC) with HYNIC NHS ester chemistry. The HYNIC–finasteride conjugate was identified by NMR, IR, MP analysis, high-resolution ESI MS ([M + H]+ m/z 507.3190, Δppm −3.9), and RP HPLC (Rt 13.9 min, > 98% purity). 99ᵐTc radiolabeling using tricine/EDDA co-ligands resulted in > 98% radiochemical purity. The radiotracer was highly stable in vitro (> 91% in PBS at 4 h; ≥ 68% in serum at 16 h) and had a logP value of −1.25 ± 0.08, with good hydrophilicity. Saturation binding assays in LNCaP cells had 5AR, with Kd and Bmax values of 3.10 ± 0.7 nM and 82.44 ± 3.2 fmol/106 cells. Biodistribution studies in LNCaP xenograft-bearing mice showed high tumor uptake (5.62% ± 0.32% ID/g at 4 h), which reduced in blocked groups (1.25% ± 0.18% ID/g). SPECT images offered selective tumor accumulation with good tumor-to-normal tissue contrast and renal clearance in tumor-bearing rabbits. These findings suggest that 99ᵐTc-HYNIC–finasteride is a promising SPECT radiotracer for noninvasive 5AR imaging in PCa.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 11-12","pages":""},"PeriodicalIF":0.9,"publicationDate":"2025-10-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145238793","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}

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Automated Manufacturing of Carbon-11 Radiopharmaceuticals Using Cassette-Based Radiosynthesizers 使用盒式放射性合成器自动制造碳-11放射性药物。

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-10-06 DOI: 10.1002/jlcr.4166

Michael L. Schulte, Adam J. Rosenberg

引用次数: 0