Article
Medicine, Research & Experimental
Jiahui Chen, Wenqing Ran, Yiman Huang, Junjie Wei, Jian Rong, Huiyi Wei, Yinlong Li, Guocong Li, Zhen Chen, Lee Collier, Nehal H. Elghazawy, Wolfgang Sippl, Ahmed Haider, Kai Liao, Chenchen Dong, Ying Li, Hao Xu, Wenpeng He, Lu Wang, Steven H. Liang
Summary: AMPA receptors play important roles in neurological disorders, but their quantification and imaging capabilities are limited. A novel compound, 6, was identified as a potential lead compound and tested using PET technology. However, it showed insufficient specific binding. Further medicinal chemistry research is needed to improve the specific binding and facilitate clinical translation.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Review
Biochemistry & Molecular Biology
Jatinder Kaur, Atul Bhardwaj, Frank Wuest
Summary: Molecular imaging probes enable early and accurate detection of disease-specific biomarkers and facilitate personalized treatment. Positron emission tomography (PET) plays a significant role in cancer detection and response monitoring. COX-2 isozyme has been identified as a crucial factor in cancer development, making it a promising biomarker.
Article
Medicine, Research & Experimental
Vu Long Tran, Aliz ee Bouleau, Herv e Nozach, Mylene Richard, Celine Chevaleyre, Steven Dubois, Dimitri Kereselidze, Bertrand Kuhnast, Michael J. Evans, Simon Specklin, Charles Truillet
Summary: Molecular imaging with PET can accurately select patients for immuno-therapies and study the impact of radiolabeling techniques on pharmacokinetics and biodistribution. This study compared two radiofluorination methods on an anti-PD-L1 Fab fragment and found that site-specific labeling better reflected the pharmacokinetic profile of the Fab.
MOLECULAR PHARMACEUTICS
(2022)
Review
Pharmacology & Pharmacy
Truong Giang Luu, Hee-Kwon Kim
Summary: TSPO plays important roles in cellular functions and its abnormal expression is associated with pathological disorders, making it a biomarker for related diseases. PET, as a non-invasive imaging technique, can detect diseases related to TSPO expression. Recent studies have focused on the development of F-18-labeled TSPO as PET tracers.
Article
Biochemistry & Molecular Biology
Valerie Weber, Lucie Arnaud, Sladjana Dukic-Stefanovic, Barbara Wenzel, Valerie Roux, Jean-Michel Chezal, Thu-Hang Lai, Rodrigo Teodoro, Klaus Kopka, Elisabeth Miot-Noirault, Winnie Deuther-Conrad, Aurelie Maisonial-Besset
Summary: This study developed new radioiodinated and radiofluorinated analogues for noninvasive imaging of mIDH1 up- and dysregulation in tumors. The radiotracers showed stability in vitro and in vivo, providing potential for further evaluations in future studies.
Article
Biochemistry & Molecular Biology
Lahu N. Chavan, Ronald Voll, Mar M. Sanchez, Jonathon A. Nye, Mark M. Goodman
Summary: This study reports a highly efficient, scalable, and expedient synthesis method for [F-18]-MDL100907, a PET radioligand. The method utilizes a cross-coupling reaction as a key step in synthesizing a F-18-labeled boron pinacol ester precursor. The method allows for the production of [F-18]-MDL100907 radioligand with excellent decay-corrected RCY within a short time frame and high molar activity, and it has been compared to [C-11]-MDL100907 in nonhuman primate brain.
ACS CHEMICAL NEUROSCIENCE
(2023)
Article
Biochemistry & Molecular Biology
Annukka Kallinen, Karine Mardon, Samuel Lane, Andrew P. Montgomery, Rajiv Bhalla, Damion H. R. Stimson, Muneer Ahamed, Gary J. Cowin, David Hibbs, Eryn L. Werry, Roger Fulton, Mark Connor, Michael Kassiou
Summary: This study synthesized fluorinated 5-azaindole compounds and evaluated their pharmacological characteristics and in vivo performance. The results showed that these compounds exhibited specific binding to CB2 receptors and demonstrated specific binding behavior in rats with neuroinflammation, suggesting the need for further evaluation of these compounds in other neuroinflammation models.
ACS CHEMICAL NEUROSCIENCE
(2023)
Article
Chemistry, Organic
Miseon Choi, Manish Kumar Mehra, Chung Whan Lee
Summary: Various indolo[2,3-b]indoles can be synthesized in one pot through a copper-catalyzed transformation of easily accessible 2-(substituted-amino)aryl)(mesityl)iodonium salts and indole derivatives. The reaction exhibits excellent functional group toleration and provides a series of indolo[2,3-b]indole derivatives in good yields. Moreover, direct access to benzoxazole derivatives can be achieved through intramolecular cyclization of 2-(substituted-amino)aryl)(mesityl)iodonium salts in the presence of copper catalyst.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Medicine, Research & Experimental
Volker Morath, Corinna Brandt, Friedrich-Christian Deuschle, Claudia T. Mendler, Birgit Blechert, Dominik Summer, Cyril Barinka, Clemens Decristoforo, Wolfgang A. Weber, Markus Schwaiger, Arne Skerra
Summary: Anticalin proteins targeting PSMA with tailored plasma half-life using PASylation technology are promising radioligands for PET imaging of xenograft tumors in mice. PET imaging using the FsC radiochelator is superior to Dfo radiochelator and adjusting the plasma half-life of Anticalin radioligands using PASylation technology can increase radioisotope accumulation within the tumor.
MOLECULAR PHARMACEUTICS
(2023)
Article
Neurosciences
Yuzhao Chen, Yilin Zhang, Qiuxuan Chen, Yuxiang Liu, Xuemin Wei, Meijian Wu, Keke Zhang, Yinghua Liu, Wei Wei
Summary: mGluR5 expression is increased in AD, and inhibition of mGluR5 can improve cognitive function, promote synaptic recovery, and alleviate A beta plaques and hyperphosphorylation. This suggests that mGluR5 may be a promising drug target for AD treatment, and inhibition of the mGluR5/PI3K-AKT pathway can alleviate AD-like pathology through activation of autophagy and anti-neuroinflammation effects.
JOURNAL OF ALZHEIMERS DISEASE
(2023)
Article
Chemistry, Medicinal
Fabrice G. Simeon, Jae-Hoon Lee, Cheryl L. Morse, Ian Stukes, Sami S. Zoghbi, Lester S. Manly, Jeih-San Liow, Robert L. Gladding, Rachel M. Dick, Xuefeng Yan, Sabrina Taliani, Barbara Costa, Claudia Martini, Federico Da Settimo, Sabrina Castellano, Robert B. Innis, Victor W. Pike
Summary: The study aimed to develop a new TSPO imaging agent with a longer half-life and low sensitivity to human genotypes. The results showed that the 3-fluoro analog exhibited the most promising potential for PET imaging applications.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Meijuan Jiang, Shuiyu Lu, Sanjay Telu, Victor W. Pike
Summary: Development of a PET radioligand for imaging PDE4D is important for drug discovery and understanding neuropsychiatric disorders. The existing radioligand, [11C]T1650, shows unstable quantification in humans, necessitating structural improvements. By formulating and optimizing an empirical equation, we successfully predicted and obtained 14 new compounds with high inhibitory potency. Eight of these compounds were deemed suitable for future radiolabeling and evaluation as PDE4D PET radioligands.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Endocrinology & Metabolism
Louise Breuil, Solene Marie, Sebastien Goutal, Sylvain Auvity, Charles Truillet, Wadad Saba, Oliver Langer, Fabien Caille, Nicolas Tournier
Summary: This study investigates differences in vulnerability to P-gp inhibition among radiolabeled substrates and emphasizes the importance of considering partial inhibition of transporter function as a primary criterion in evaluating the sensitivity of radiolabeled substrates to detect moderate but physiologically-relevant changes in transporter function in vivo.
JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM
(2021)
Article
Chemistry, Applied
Shu-Min Nie, Xu Zhang, Zhi-Xin Wang, Gui-Fa Su, Cheng-Xue Pan, Dong-Liang Mo
Summary: A variety of functionalized indazole compounds were successfully synthesized through a transition metal-free radical strategy, and the reaction mechanism was investigated. The reaction exhibited high yields and tolerated various sensitive functional groups.
ADVANCED SYNTHESIS & CATALYSIS
(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
Biochemical Research Methods
Jun Young Park, Jeongmin Son, Mijin Yun, Simon M. Ametamey, Joong-Hyun Chun
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
(2018)
Article
Chemistry, Organic
Young-Do Kwon, Jeongmin Son, Mijin Yun, Joong-Hyun Chun
TETRAHEDRON LETTERS
(2018)
Article
Chemistry, Organic
Young-Do Kwon, Jeongmin Son, Joong-Hyun Chun
JOURNAL OF ORGANIC CHEMISTRY
(2019)
Article
Radiology, Nuclear Medicine & Medical Imaging
Anton Lindberg, Shuiyu Lu, Sangram Nag, Magnus Schou, Jeih-San Liow, Sami S. Zoghbi, Michael P. Frankland, Robert L. Gladding, Cheryl L. Morse, Akihiro Takano, Nahid Amini, Charles S. Elmore, Yong Sol Lee, Robert B. Innis, Christer Halldin, Victor W. Pike
NUCLEAR MEDICINE AND BIOLOGY
(2019)
Article
Radiology, Nuclear Medicine & Medical Imaging
Dongwoo Kim, Joong-Hyun Chun, Se Hoon Kim, Ju Hyung Moon, Seok-Gu Kang, Jong Hee Chang, Mijin Yun
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2019)
Article
Chemistry, Multidisciplinary
Jimmy E. Jakobsson, Shuiyu Lu, Sanjay Telu, Victor W. Pike
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2020)
Article
Cell Biology
Shuiyu Lu, Mohammad B. Haskali, Kevin M. Ruley, Nicolas J-F Dreyfus, Susan L. DuBois, Soumen Paul, Jeih-San Liow, Cheryl L. Morse, Aneta Kowalski, Robert L. Gladding, Jeremy Gilmore, Adrian J. Mogg, S. Michelle Morin, Peter J. Lindsay-Scott, J. Craig Ruble, Nancy A. Kant, Sergey Shcherbinin, Vanessa N. Barth, Michael P. Johnson, Maria Cuadrado, Enrique Jambrina, Andrew J. Mannes, Hugh N. Nuthall, Sami S. Zoghbi, Cynthia D. Jesudason, Robert B. Innis, Victor W. Pike
SCIENCE TRANSLATIONAL MEDICINE
(2020)
Article
Chemistry, Organic
Young-Do Kwon, Min Ho Jeon, Nam Kyu Park, Jeong Kon Seo, Jeongmin Son, Young Hoon Ryu, Sung You Hong, Joong-Hyun Chun
Article
Chemistry, Organic
Min Ho Jeon, Young-Do Kwon, Min Pyeong Kim, Gianluca Bartolini Torres, Jeong Kon Seo, Jeongmin Son, Young Hoon Ryu, Sung You Hong, Joong-Hyun Chun
Summary: The study presents a successful synthesis of various sulfamoyl [F-18]fluorides using an F-18/F-19 isotopic exchange approach, improving synthetic efficiency with radiochemical yields up to 97%. This late-stage labeling protocol offers an efficient route to diversify the chemical library possessing sulfamoyl functionalities by incorporating nucleophilic F-18 within nitrogen-containing sulfur(VI) frameworks.
Article
Multidisciplinary Sciences
Jae Bin Lee, Gun Ha Kim, Ji Hwan Jeon, Seo Yeong Jeong, Soochan Lee, Jaehyun Park, Doyoung Lee, Youngkook Kwon, Jeong Kon Seo, Joong-Hyun Chun, Seok Ju Kang, Wonyoung Choe, Jan-Uwe Rohde, Sung You Hong
Summary: The authors present a transition-metal-free, radical relay pi-extension approach to produce N-doped polycyclic aromatic compounds directly from simple azines and cyclic iodonium salts. This method offers a solution to the limitation of low reactivity in unactivated azines.
NATURE COMMUNICATIONS
(2022)
Article
Radiology, Nuclear Medicine & Medical Imaging
Dongwoo Kim, Joong Hyun Chun, Ju Hyeon Yi, Hae Young Ko, Jee-In Chung, Misu Lee, Yongmin Mason Park, Min-Ho Nam, Jisu Kim, Seon Yoo Kim, Youngjoo Park, Ju Hyung Moon, Seok-Gu Kang, Jong Hee Chang, C. Justin Lee, Se Hoon Kim, Mijin Yun
Summary: C-11-ACE PET/CT is an imaging biomarker that can characterize reactive astrogliosis in different types of gliomas. High C-11-ACE uptake is associated with high-grade IDH1-wt tumors, allowing differentiation from high-grade IDH1-mt and low-grade gliomas. Low C-11-ACE uptake in ODs is advantageous in overcoming the limitations of radiolabeled amino acid tracers.
CLINICAL NUCLEAR MEDICINE
(2022)
Article
Chemistry, Medicinal
Meijuan Jiang, Shuiyu Lu, Sanjay Telu, Victor W. Pike
Summary: Development of a PET radioligand for imaging PDE4D is important for drug discovery and understanding neuropsychiatric disorders. The existing radioligand, [11C]T1650, shows unstable quantification in humans, necessitating structural improvements. By formulating and optimizing an empirical equation, we successfully predicted and obtained 14 new compounds with high inhibitory potency. Eight of these compounds were deemed suitable for future radiolabeling and evaluation as PDE4D PET radioligands.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Medicine, Research & Experimental
Su Bin Kim, In Ho Song, Seon Yoo Kim, Hae Young Ko, Hee Seup Kil, Dae Yoon Chi, Frederik L. Giesel, Klaus Kopka, Alexander Hoepping, Joong-Hyun Chun, Hyun Soo Park, Mijin Yun, Sang Eun Kim
Summary: Several radiolabeled PSMA-targeted agents have been developed for detecting prostate cancer and targeted radionuclide therapy. This study characterized the pharmacokinetics and radiation dose of [18F]PSMA-1007 in prostate tumor-bearing mice. The kidney showed the highest accumulation of [18F]PSMA-1007, and the concentration in the tumor reached its peak at 112 min after injection. Treatment with a PSMA inhibitor significantly decreased [18F]PSMA-1007 uptake in the tumor.
MOLECULAR PHARMACEUTICS
(2022)
Article
Chemistry, Organic
Min Pyeong Kim, Hojin Cho, Swatilekha Kayal, Min Ho Jeon, Jeong Kon Seo, Jeongmin Son, Jinsil Jeong, Sung You Hong, Joong-Hyun Chun
Summary: We describe a direct radiofluorosulfurylation method that synthesizes 18F-labeled fluorosulfuryl derivatives from phenols and amines using an [18F]FSO2+ transfer agent generated in situ. Nucleophilic radiofluorination can be achieved even in a hydrous organic medium, eliminating the need for azeotropic drying and the use of cryptands. This unprecedented and operationally simple isotopic functionalization enables the reliable production of potential radiotracers for positron emission tomography, providing easy access to SuFEx radiochemistry.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Organic
Qunchao Zhao, Jean M. Etersque, Shuiyu Lu, Sanjay Telu, Victor W. Pike
Summary: In this study, we investigated the use of aryliodonium precursors for copper-free labeling of PET tracers with fluorine-18. We found that regioisomeric F-18-fluoroarenes can be formed in certain labeling methods. The reaction between aryliodonium ylides derived from Meldrum's acid with para electron-donating groups and [F-18]-fluoride in acetonitrile produces regioisomeric F-18-fluoroarenes via a competing aryne pathway. The formation of regioisomers is decreased or absent in DMF. It is recommended to analytically check for the absence of the F-18-regioisomer in any specific PET tracer radiosynthesis using these or similar methods.
Article
Chemistry, Organic
Faiza Diaba, Gisela Trenchs
Summary: The first violet light-mediated synthesis of gamma- and delta-lactams from N-alkenyl trichloroacetamides is reported in this paper. The reactions are conducted in tetrahydrofuran or 2-methyltetrahydrofuran as the sole solvent without catalysts or additives, under non-anhydrous conditions in an air atmosphere where the solvent serves as the radical initiator.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Feroze Hussain, Sajjad Ahmed, Ashiq Hussain Padder, Qazi Naveed Ahmed
Summary: This study reports a novel and efficient one-pot synthesis method for mixed phosphorotrithioates, which does not require supplementary additives and shows broad applicability.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Hyunjin Oh, Ikyon Kim
Summary: A new 1,2,4-triazole-pyrrolo[1,2-a]pyrazine hybrid system, 6-acylpyrrolo[1,2-a][1,2,4]triazolo[5,1-c]pyrazine, was synthesized using a catalyst-free method. This method involved sequential exposure of pyrrole-2-carbonitrile-derived substrates to DMF-DMA and acyl hydrazide, resulting in the formation of acylated pyrazine and 1,2,4-triazole rings, enabling the installation of various substituents at specific positions on the core skeleton.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Ming Yan, Si-fan Wang, Yong-po Zhang, Jin-zhong Zhao, Zhuo Tang, Guang-xun Li
Summary: Here we developed an efficient photocatalytic approach for the convenient preparation of sulfinamides. The reaction allows for the gram-scale preparation of sulfinamides and the one-pot synthesis of various sulfonyl amides.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Farzaneh Bandehali-Naeini, Zahra Tanbakouchian, Noushin Farajinia-Lehi, Nicolas Mayer, Morteza Shiri, Martin Breugst
Summary: Two tandem catalytic systems were developed for the synthesis of novel 3,4-disubstituted maleimides using the same Ugi adducts. Different maleimide structures can be synthesized using either Pd or Cu catalysis.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Tanya Raghava, Anjan Chattopadhyay, Subhadeep Banerjee, Nivedita Sarkar
Summary: Amine substitution of two ortho fluorine atoms of tetrafluoroterephthalonitrile through SNAr chemistry is easily achievable. But further fluorine substitution is only possible under forcing conditions, yielding valuable fluorophores for bioimaging.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Review
Chemistry, Organic
Anju Chadha, Santosh Kumar Padhi, Selvaraj Stella, Sowmyalakshmi Venkataraman, Thangavelu Saravanan
Summary: Alcohol dehydrogenases are enzymes that use cofactors for oxidation or reduction reactions of alcohols or carbonyl compounds. They are utilized in green chemistry and have applications in the production of pharmaceuticals. Recombinant enzymes have solved the challenge of producing purified enzymes in large quantities. Engineered alcohol dehydrogenases have been used in asymmetric synthesis in industry. Various methods have been established for regenerating expensive cofactors to make the enzymatic process more efficient and economically viable.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)