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radiolabeling of lacosamide using highly purified rhenium-188 as a prospective brain theranostic agent

Nuclear Science and Techniques 2020年第10期31卷 105-114页

作者： H.A.El-Sabagh M.I.Aydia A.M.Amin K.M.El-Azony Labeled Compound Department Radioisotopes Production DivisionHot Laboratory CenterAtomic Energy AuthorityP.O.Box 13759 CairoEgypt Radioactive Isotopes and Generators Department Radioisotopes Production DivisionHot Laboratory CenterAtomic Energy AuthorityP.O.Box 13759 CairoEgypt

Rhenium-188 is prospectively effective for both diagnosis and radiotherapy as it appropriately emits gamma rays and beta ***(LCM)is a newly approved antiepileptic medication for focal drug-resistant ***-188 was separated with high elution yield and high purity using the new 188W/188Re generator based on the ZrSiW gel matrix.188Re-LCM was prepared with high radiochemical yield and high *** of 188Re-LCM in normal Swiss albino mice was investigated to determine its utility as a potential brain therapy *** 188W/188Re generator was used to obtain 188Re based on the ZrSi188W gel matrix,and the chemical,radiochemical,and radionuclidic purity of the obtained 188Re was determined using inductively coupled plasma optical emission spectrometry(ICP-AES),a paper chromatography technique,and high-purity germanium(HPGe)detection,respectively,to assess its validity for LCM *** factors,such as the pH,reaction time,and LCM quantity,were therefore studied in order to improve the yield and purity of 188Re-LCM,as determined by various chromatographic techniques such as electrophoresis,thin layer chromatography(TLC),and highpressure liquid chromatography(HPLC).188Re was obtained with a high elution yield(75±3%)and a low 188W breakthrough(0.001±0.0001%).The maximum radiochemical yield of 188Re-LCM(87.5±1.8%)was obtained using 50 ll LCM(4 mM),250 ll stannous chloride(4.4 mM)at pH 4,100 ll 188Re(37 MBq),within 30 min,at room temperature(25±3C),as determined by TLC,electrophoresis,and HPLC *** analysis showed that 188Re-LCM was primarily localized in the brain(5.1%)with a long residence time(240 min).

关键词： Lacosamide 188Re 188W/188Re generator radiolabeling

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Expression and radiolabeling of Cas9 protein

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Nuclear Science and Techniques 2017年第1期28卷 74-79页

作者： Qing-Long Yan Hua-Ting Kong Kai Xia Yu Zhang Ali Aladlbahi Ji-Ye Shi Li-Hua Wang Chun-Hai Fan Yun Zhao Ying Zhu Key Laboratory of Bio-Resources and Eco-Environment Ministry of Education College of Life Sciences Sichuan University Chengdu 610064 China Division of Physical Biology and Bioimaging Center CAS Key Laboratory of Interfacial Physics and TechnologyShanghai Institute of Applied Physics Chinese Academy of Sciences Jiading Campus Shanghai 201800 China Chemistry Department King Saud University Riyadh 11451Saudi Arabia UCB Pharma Slough SL1 3WE UK

As a robust platform for genome editing,CRISPR/Cas9 is currently being explored for engineering biology or therapeutics,yet means for quantitative detection of Cas9 proteins remain to be fully ***,we expressed Cas9 proteins and developed a novel detection method that traced Cas9 based on radiolabeled *** optimizing the reaction conditions of reaction time,temperature and cycles,we obtained ^(125)I-Cas9 of high labeling *** prepared ^(125)I-Cas9 was stable in various media and preserved excellent genome editing ***,our strategy provides a convenient and efficient tool for further tracing biological behaviors of Cas9 proteins in living systems.

关键词： Cas9 radiolabeling 125I labeling yield Stability

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Natural product-based radiopharmaceuticals:Focus on curcumin and its analogs,flavonoids,and marine peptides

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Journal of Pharmaceutical Analysis 2022年第3期12卷 380-393页

作者： Hendris Wongso Labeled Compound and Radiometry Division Center for Applied Nuclear Science and TechnologyNational Nuclear Energy AgencyBandung40132Indonesia

Natural products provide a bountiful supply of pharmacologically relevant precursors for the development of various drug-related molecules,including ***,current knowledge regarding the importance of natural products in developing new radiopharmaceuticals remains *** date,several radionuclides,including gallium-68,technetium-99m,fluorine-18,iodine-131,and iodine-125,have been extensively studied for the synthesis of diagnostic and therapeutic *** availability of various radiolabeling methods allows the incorporation of these radionuclides into bioactive molecules in a practical and efficient *** the radiolabeling methods,direct radioiodination,radiometal complexation,and halogenation are generally suitable for natural products owing to their simplicity and *** review highlights the pharmacological benefits of curcumin and its analogs,flavonoids,and marine peptides in treating human pathologies and provides a perspective on the potential use of these bioactive compounds as molecular templates for the design and development of new ***,this review provides insights into the current strategies for labeling natural products with various radionuclides using either direct or indirect methods.

关键词： Natural products Radiopharmaceuticals radiolabeling Curcumin Flavonoids Marine peptides

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Isolation of ^(212)Pb from natural thorium for targeted alpha-therapy

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Chinese Chemical Letters 2022年第7期33卷 3474-3477页

作者： Junyi Chen Mengxin Xu Yu Liu Dongban Duan Yuxiang Han Zhibo Liu Beijing National Laboratory for Molecular Sciences Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental ScienceCollege of Chemistry and Molecular EngineeringPeking UniversityBeijing 100871China Peking-Tsinghua Center for Life Sciences Peking UniversityBeijing 100871China

Targeted alpha-therapy(TAT) is increasingly attractive due to its extraordinary antitumor ***,the supply of α-emitters for TAT is insufficient and under control by a limited number of countries.^(212)Pb is a promising α-emitter with an optimal half-life(10.6 h) and favored decay *** interest,^(212)Pb can be extracted directly from natural thorium,which may be abundant in the mining waste of rare-earth,uranium,***,radioactive thorium waste has been a longstanding environmental challenge that needs immediate *** an on-demand and facile process to isolate ^(212)Pb from natural thorium would be ideal to meet the above challenges,yet is *** theory,the ratio of ^(212)Pb tonatTh is below 10^(-13)in commercially available thorium *** a pilot study,2.2 MBq of ^(212)Pb was successfully extracted from a 5 L solution of thorium nitrate by using a Pb-selective *** radiochemical purity of ^(212)Pb is over 99.9% according to gamma-ray *** purified^(212)Pb was applied to radiolabel a couple of peptides used in clinics(***,TATE and FAPI-04),and the radiochemical yields are>85%.Of note,^(212)Pb can be repeatedly separated from the thorium solution every 2 *** summary,a practical and scalable method was developed to isolate^(212)Pb for potentially clinical use,which may be of great importance as it does not require either cyclotron or nuclear reactor.

关键词： ^(212)Pb Targeted alpha-therapy radiolabeling Radionuclide generator Solid-phase extraction

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Peptides Radiofluorination: Main Methods and Highlights

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International Journal of Organic Chemistry 2022年第4期12卷 161-172页

作者： Ana Carolina A. Bispo Fernanda A. F. Almeida Juliana B. Silva Marcelo Mamede Radiopharmaceutical Research and Production Unit Nuclear Technology Development Center Belo Horizonte Brazil Anatomy and Imaging Department Faculty of Medicine Federal University of Minas Gerais Belo Horizonte Brazil

Peptides have an important role in organism and its high quantity present in tumors leading to development of radiolabeled peptides for tumor-specific imaging. Once the traditional methodologies used for radiofluorination do not work with peptides, due to their harsh conditions, other radiolabeling strategies had to be developed to supply the need. Direct radiofluorination is either an inefficient method, and the use of bidirectional groups, or prosthetic groups, is needed to enable the binding between the radionuclide fluorine-18 and a peptide functionalized. New peptides radiolabeling strategies have been developed sourcing increase the synthesis yield, its chemoselectivity, and the binding stability, and reduce the total process time and the number of steps required. The progress of radiofluorination methodologies led to development of the amidation, acylation, imidation, and alkylation techniques, the use of thiol groups, photochemical conjugation, chemoselective reactions, and “click chemistry”, in addition to use of FDG molecule and heteroatoms as linkers. This paper presents the main strategies used for peptides radiofluorination, presenting their positive and negative points, and the prosthetic groups most used in each method.

关键词： Radiofluorination radiolabeling Peptides Prosthetic Groups Fluorine-18

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Radiosynthesis of [^(18)F]ArylSCF2H Using Aryl Boronic Acids, S-(Chlorofluoromethyl) benzenesulfonothioate and [^(18)F]Fluoride

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CCS Chemistry 2021年第7期3卷 1921-1928页

作者： Qunchao Zhao Patrick G.Isenegger Thomas C.Wilson Jeroen BISap Florian Guibbal Long Lu Véronique Gouverneur Qilong Shen Key Laboratory of Organofluorine Chemistry Center for Excellence in Molecular Synthesis Shanghai Institute of Organic ChemistryUniversity of Chinese Academy of SciencesChinese Academy of SciencesShanghai 200032 Chemistry Research Laboratory University of OxfordOxford OX13TA Shanghai Institute of Organic Chemistry Chinese Academy of SciencesShanghai 200032

Herein,we report a mild and practical protocol for the copper-catalyzed chlorofluoromethylthiolation of(hetero)aryl boronic acids with the novel reagent *** resulting products are amenable to halogen-exchange^(18)F-fluorination with cyclotronproduced[^(18)F]fluoride affording[^(18)F]*** process highlights the combined value of reagent development and(hetero)aryl boron precursors for radiochemistry by adding the[^(18)F]SCF2H group to the list of^(18)F-motifs within reach for positron emission tomography studies.

关键词： chlorofluoromethylthiolation boron reagent PET fluorine radiolabeling

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