Review
Chemistry, Multidisciplinary
Yunze Wang, Qingyu Lin, Hongcheng Shi, Dengfeng Cheng
Summary: Positron emission tomography (PET) molecular imaging technology is a critical tool for evaluating biological and biochemical processes. Fluorine-18 has favorable characteristics for labeling and molecular imaging, making it significant in radiochemistry and radiopharmaceutics. The development of new reagents and catalysts has led to rapid growth in F-18 labeling methods over the past decades.
FRONTIERS IN CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Monica Rivas, Sashi Debnath, Sachin Giri, Yusuf M. Noffel, Xiankai Sun, Vladimir Gevorgyan
Summary: We describe a one-pot formal alkene carboradiofluorination reaction that utilizes easily accessible alkenes as both prosthetic group precursors and coupling partners. This methodology offers a rapid and mild fluorine-18 (18F) radiochemical approach for positron emission tomography (PET) imaging probe development. The methods were successfully applied to the synthesis of over 30 analogues of bioactive molecules and demonstrated good radiochemical conversion in radiolabeling medicinally relevant small molecules.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2023)
Article
Chemistry, Multidisciplinary
Monica Rivas, Sashi Debnath, Sachin Giri, Yusuf M. Noffel, Xiankai Sun, Vladimir Gevorgyan
Summary: We report the first one-pot formal alkene carboradiofluorination reaction using easily accessible alkenes as both precursors and partners, which provides a mild and robust fluorine-18 radiochemical approach for PET imaging probe development. A new class of prosthetic groups for PET imaging probe synthesis was isolated as iodofluorinated intermediates, and the method was successfully applied to produce over 30 analogues of bioactive molecules. The protocol was further optimized for future (pre)clinical translation and automation in multistep radiochemical reactions.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Joseph Therriault, Andrea L. Benedet, Tharick A. Pascoal, Melissa Savard, Nicholas J. Ashton, Mira Chamoun, Cecile Tissot, Firoza Lussier, Min Su Kang, Gleb Bezgin, Tina Wang, Jaime Fernandes-Arias, Gassan Massarweh, Paolo Vitali, Henrik Zetterberg, Kaj Blennow, Paramita Saha-Chaudhuri, Jean-Paul Soucy, Serge Gauthier, Pedro Rosa-Neto
Summary: This study assessed multiple methods for determining an optimal cutoff for F-18-AZD4694 PET positivity, with good convergence among different approaches. The findings suggest that a threshold of 1.55 SUVR may have reliable discriminative accuracy for amyloid-beta positivity on PET imaging.
JOURNAL OF NUCLEAR MEDICINE
(2021)
Article
Nanoscience & Nanotechnology
Chunmei Lu, Ke Li, Hongjie Xi, Di Hua, Huirong Li, Feng Gao, Ling Qiu, Jianguo Lin
Summary: In this study, dual-targeting radiotracers with legumain-mediated self-assembly were developed for positron emission tomography (PET) imaging of tumors. The radiotracers showed enhanced retention in legumain-overexpressed tumors, indicating their potential application in clinical settings.
ACS APPLIED MATERIALS & INTERFACES
(2023)
Article
Chemistry, Multidisciplinary
Rocio Garcia-Vazquez, Umberto M. Battisti, Jesper T. Jorgensen, Vladimir Shalgunov, Lars Hvass, Daniel L. Stares, Ida N. Petersen, Francois Crestey, Andreas Loeffler, Dennis Svatunek, Jesper L. Kristensen, Hannes Mikula, Andreas Kjaer, Matthias M. Herth
Summary: In this study, a simple, scalable, and reliable direct F-18 labeling procedure was developed and successfully applied to create a tetrazine-based imaging agent for pretargeting. The tracer showed promising characteristics that may qualify it for future clinical translation.
Article
Chemistry, Analytical
Xinxin Wang, Jianguo Xu, Panzhu Qin, Chao Yan, Guodong Liu, Wei Chen
Summary: The isothermal method described utilizes PTA-MBs to assemble DNA nanostructures and achieve signal amplification for quantification of TdT activity, demonstrating excellent selectivity and practical applicability in direct/absolute quantification in real biological samples.
ANALYTICA CHIMICA ACTA
(2021)
Article
Chemistry, Organic
German Fuentes, Maria F. Garcia, Hugo Cerecetto, Guzman alvarez, Marcos Couto, Angel H. Romero
Summary: Favipiravir has emerged as an important selective antiviral against COVID-19, but its conventional synthesis methods have limitations. This study presents a one-step protocol for the synthesis of favipiravir using a direct fluorination reaction, which is simple, economical, eco-friendly, and scalable. The use of ionic liquid BF4-BMIM helps to overcome the chemical limitations of the substrate and improve the yield of favipiravir to 50%.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2023)
Article
Chemistry, Physical
Pin Chen, Siyuan Di, Xiaoqing Qiu, Shukui Zhu
Summary: Highly efficient visible-light-active catalysts F-TiO2/g-C3N4 were synthesized via a one-step-calcination method, exhibiting excellent separation and migration of photoelectron-hole pairs and effective degradation of flame retardants and antibiotics.
APPLIED SURFACE SCIENCE
(2022)
Article
Neurosciences
Yanxiao Li, Yee Ling Ng, Manish D. Paranjpe, Qi Ge, Fengyun Gu, Panlong Li, Shaozhen Yan, Jie Lu, Xiuying Wang, Yun Zhou
Summary: This study aimed to improve the statistical power in detecting changes in brain glucose metabolism, amyloid, and tau deposition in Alzheimer's disease studies by using a reference tissue-based quantification approach. The results showed that the tracer-specific reference tissue improved the detection of PET SUVR changes, which is beneficial for early diagnosis, disease progression monitoring, and therapeutic response in Alzheimer's disease.
HUMAN BRAIN MAPPING
(2022)
Article
Biochemical Research Methods
Yingqing Lu, Yingfang He, Roger Schibli, Linjing Mu, R. Michael van Dam
Summary: Copper-mediated radiofluorination has great potential in the synthesis of PET radioligands. We demonstrated the feasibility of Cu-mediated radiosynthesis on a high-throughput microdroplet platform and optimized the reaction conditions. By utilizing microscale conditions, we achieved higher radiochemical yield and excellent radiochemical purity and molar activity. We also successfully translated these optimized conditions to a vial-based method, expanding the applicability of the synthesis approach.
Article
Chemistry, Medicinal
Chunmei Lu, Xiuting Wang, Qiqi Wang, Lixia Zhang, Jianguo Lin, Ling Qiu
Summary: Legumain is overexpressed in several cancers and serves as an important biomarker for cancer diagnosis. In this study, a novel radioactive tracer [F-18]SF-AAN was designed and synthesized for positron emission tomography (PET) imaging, targeting legumain. The tracer showed specificity in detecting legumain activity in vitro and in vivo, making it a promising tool for the diagnosis of legumain-related diseases.
Article
Oncology
Lidija Antunovic, Alessia Artesani, Alessandro Vigano, Arturo Chiti, Armando Santoro, Martina Sollini, Silvia D. Morbelli, Rita De Sanctis
Summary: This study aimed to examine brain metabolic patterns on [F-18]Fluorodeoxyglucose ([F-18]FDG) positron emission tomography (PET) in breast cancer (BC), comparing patients with tension-type headache (TTH), migraine (MiG), and those without headache. The results showed that headache patients exhibited hypometabolism in specific brain regions before neoadjuvant chemotherapy (NAC) and headache patients with a good response to NAC showed hypermetabolic brain regions in the anterior medial frontal cortex.
Article
Chemistry, Multidisciplinary
Zetan Fan, Jian Zhao, Xin Chai, Lele Li
Summary: The study introduces a DNA-based fluorescent reporter that can detect the activity of two enzymes, TE and APE1, which are crucial for tumor progression and drug treatment. The system allows for in vivo imaging of the enzymatic activities and specific tumor imaging through a dual lock-and-key strategy.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Editorial Material
Radiology, Nuclear Medicine & Medical Imaging
Jonas Werner, Hannes Grunig, Hannah Loher, Stefan Fischli, Klaus Strobel, Corinna Wicke
Summary: We report a case of a 68-year-old woman with a tibial tumor and fatigue, which was diagnosed as a brown tumor secondary to severe primary hyperparathyroidism. F-18-fluorocholine PET/CT was used to localize the parathyroid adenoma and brown tumors, which were confirmed by unilateral neck exploration. After parathyroidectomy, the patient's symptoms improved with normalization of serum calcium and parathyroid hormone levels.
CLINICAL NUCLEAR MEDICINE
(2023)
Article
Oncology
Qingzhu Liu, Lei Jiang, Ke Li, Hang Li, Gaochao Lv, Jianguo Lin, Ling Qiu
Summary: The study assessed a non-blocking nanobody tracer's specificity and dynamic monitoring property to PD-L1, demonstrating its high sensitivity and specificity in monitoring PD-L1 expression. The tracer showed potential for guiding immunotherapy and immunochemotherapy for refractory cancers.
CANCER IMMUNOLOGY IMMUNOTHERAPY
(2021)
Article
Chemistry, Multidisciplinary
Yirui Guo, Dingyao Gao, Yinfei Chen, Yu Zhang, Liping Chen, Yong Mao, Chunjing Yu, Ling Qiu, Jianguo Lin
Summary: F-18-GLNTGT, a PET probe with good specificity targeting PSMA, shows promise in the treatment of prostate cancer.
Article
Chemistry, Multidisciplinary
Ling Qiu, Ke Li, Wenyi Dong, Yann Seimbille, Qingzhu Liu, Feng Gao, Jianguo Lin
Summary: The study presents a novel PET tracer [F-18]1 targeting cancer-associated receptors, which forms nanoparticles through self-assembly and enhances retention and uptake in target tissues, showing promise for accurately detecting BR-positive cancers. The tumor microenvironment responsive self-assembly nanoplatform holds potential for developing other smart molecular probes.
Article
Chemistry, Multidisciplinary
Yuxuan Hu, Yinxing Miao, Junya Zhang, Yinfei Chen, Ling Qiu, Jianguo Lin, Deju Ye
Summary: This study presents an enzyme-activatable probe for high sensitivity bimodal imaging of tumors, utilizing an enzyme-induced reaction and coassembly strategy. The method significantly enhances NIR FL and radioactivity imaging sensitivity, facilitating the differentiation of tumor foci from normal tissues in vivo.
Article
Chemistry, Multidisciplinary
Jianguo Lin, Dingyao Gao, Shijie Wang, Gaochao Lv, Xiuting Wang, Chunmei Lu, Ying Peng, Ling Qiu
Summary: In this paper, a stimuli-responsive bioorthogonal reaction scaffold (SF) was reported for controlling in situ self-assembly. By integrating different substrates, two radioactive PET tracers with high stability and clear tumor PET signal were designed to detect enzyme activity.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2022)
Article
Chemistry, Medicinal
Chunmei Lu, Xiuting Wang, Qiqi Wang, Lixia Zhang, Jianguo Lin, Ling Qiu
Summary: Legumain is overexpressed in several cancers and serves as an important biomarker for cancer diagnosis. In this study, a novel radioactive tracer [F-18]SF-AAN was designed and synthesized for positron emission tomography (PET) imaging, targeting legumain. The tracer showed specificity in detecting legumain activity in vitro and in vivo, making it a promising tool for the diagnosis of legumain-related diseases.
Article
Medicine, Research & Experimental
Jingyun Ren, Shiyu Zhu, Guojin Zhang, Xiaoyue Tan, Ling Qiu, Jianguo Lin, Lei Jiang
Summary: In this study, a PET probe named 68Ga-DOTA-R01-MG was developed for imaging alpha v beta 6-positive lung cancer, which demonstrated excellent stability and specific binding to the target. The probe showed rapid and good tumor uptake and clearance in animal models, indicating its potential as a promising PET tracer for imaging alpha v beta 6-positive lung cancer.
MOLECULAR PHARMACEUTICS
(2022)
Article
Chemistry, Multidisciplinary
Ruibing An, Lingjun Liu, Shixuan Wei, Zheng Huang, Ling Qiu, Jianguo Lin, Hong Liu, Deju Ye
Summary: This study presents a glioma targeting and redox activatable theranostic nanoprobe for on-demand synergistic chemotherapy/photodynamic therapy (Chemo-PDT) of orthotopic gliomas. The nanoprobe disassembles and releases small molecules upon reduction by endogenous glutathione, allowing for synergistic Chemo-PDT. Additionally, the nanoprobe is capable of noninvasive detection and monitoring of orthotopic brain tumor growth. This research highlights the potential of targeted and activatable nanoagents for combinational cancer theranostics.
Correction
Chemistry, Multidisciplinary
Jianguo Lin, Dingyao Gao, Shijie Wang, Gaochao Lv, Xiuting Wang, Chunmei Lu, Ying Peng, Ling Qiu
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2022)
Article
Chemistry, Medicinal
Liang Xu, Lixia Zhang, Beibei Liang, Shiyu Zhu, Gaochao Lv, Ling Qiu, Jianguo Lin
Summary: Immunotherapy targeting PD-1/PD-L1 pathway has been effective in treating tumors, but response rate is not satisfactory. Studies have shown a positive correlation between PD-L1 expression and treatment response. Accurate measurement of PD-L1 expression can improve patient selection and overall treatment outcomes.
Article
Chemistry, Multidisciplinary
Bo Hu, Sudong Kong, Yuhua Weng, Deyao Zhao, Abid Hussain, Qingze Jiao, Shijing Zhan, Ling Qiu, Jianguo Lin, Minhao Xie, Bo Li, Yuanyu Huang
Summary: With the development of siRNA delivery strategy, more siRNA therapeutics for tumor treatment have emerged. However, efficient delivery of siRNA to tumor tissues remains challenging. Albumin, as an ideal carrier, can deliver hydrophobic agents into tumor tissue due to its high concentration and long circulation time.
CHINESE CHEMICAL LETTERS
(2023)
Article
Nanoscience & Nanotechnology
Chunmei Lu, Ke Li, Hongjie Xi, Di Hua, Huirong Li, Feng Gao, Ling Qiu, Jianguo Lin
Summary: In this study, dual-targeting radiotracers with legumain-mediated self-assembly were developed for positron emission tomography (PET) imaging of tumors. The radiotracers showed enhanced retention in legumain-overexpressed tumors, indicating their potential application in clinical settings.
ACS APPLIED MATERIALS & INTERFACES
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Shiyu Zhu, Beibei Liang, Yuxuan Zhou, Yinfei Chen, Jiayu Fu, Ling Qiu, Jianguo Lin
Summary: A novel peptide-based radiotracer for accurately detecting PD-L1 expression and guiding cancer immunotherapy was developed. The radiotracer, [Ga-68]/[F-18]AlF-NOTA-IMB, showed high affinity to PD-L1 and could sensitively detect changes in PD-L1 expression induced by immunotherapy using PET imaging.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2023)
Article
Biochemistry & Molecular Biology
Sudong Kong, Xiaoqing Gao, Qianhui Wang, Jianguo Lin, Ling Qiu, Minhao Xie
Summary: A novel dithiomaleimides-based tetra-antennary GalNAc conjugate was successfully developed for efficient siRNA delivery and good traceability. It can be easily constructed through three click-type reactions and has comparable siRNA delivery efficiency to the GalNAc L96 standard. In addition, the internal DTMs provide highly fluorescent emission, benefiting delivery tracking and reducing the cost and side effects of extra addition of hydrophobic dye molecules.
Article
Materials Science, Biomaterials
Qiqi Wang, Chunmei Lu, Ke Li, Yongmei Xia, Ling Qiu, Jianguo Lin
Summary: A legumain-targeted therapeutic agent [I-131]MAAN was synthesized and showed high radiochemical purity. It exhibited specificity and cytotoxicity against legumain-positive cancer cells. Cerenkov imaging with [I-131]MAAN produced clear tumor images, and TRT using this agent significantly inhibited tumor growth without obvious toxicity.
JOURNAL OF MATERIALS CHEMISTRY B
(2022)