Article
Biochemistry & Molecular Biology
Xiang Zhang, Falguni Basuli, Zhen-Dan Shi, Swati Shah, Jianfeng Shi, Amelia Mitchell, Jianhao Lai, Zeping Wang, Dima A. Hammoud, Rolf E. Swenson
Summary: In this study, a series of fluorine-18-labeled L-rhamnose derivatives were developed as potential PET tracers for various fungal and bacterial strains. The tracer showed good stability and renal clearance in mice, with minimal tissue and skeletal uptake and a low background signal in healthy mice.
Article
Clinical Neurology
Yuko Koshimori, Michael D. Cusimano, Erica L. Vieira, Pablo M. Rusjan, Stephen J. Kish, Neil Vasdev, Sho Moriguchi, Isabelle Boileau, Thomas Chao, Zahra Nasser, M. Ishrat Husain, Khunsa Faiz, Joeffre Braga, Jeffrey H. Meyer
Summary: Traumatic brain injury (TBI) is common, but the reason behind persisting symptoms in some patients is unknown. Astrogliosis, a response to brain injury, may be a potential therapeutic target, but its presence in TBI patients with persistent symptoms has not been confirmed.
Article
Chemistry, Multidisciplinary
Jay S. Wright, Richard Ma, E. William Webb, Wade P. Winton, Jenelle Stauff, Kevin Cheng, Allen F. Brooks, Melanie S. Sanford, Peter J. H. Scott
Summary: This report presents the development of a Zn(OTf)(2)-mediated method for converting alpha-tertiary haloamides to the corresponding alpha-tertiary fluoroamides. Under optimized conditions, high radiochemical conversion can be achieved. This method has been successfully applied to prepare various model radiofluorides.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Biochemistry & Molecular Biology
Thu Hang Lai, Magali Toussaint, Rodrigo Teodoro, Sladjana Dukic-Stefanovic, Mathias Kranz, Winnie Deuther-Conrad, Rares-Petru Moldovan, Peter Brust
Summary: The research focuses on developing a PET radiotracer for monitoring the expression and occupancy of the non-dopaminergic target A(2A) receptor in Parkinson's disease therapy. Novel fluorinated analogs are designed and evaluated in preclinical studies, showing specific in vitro binding to A(2A)R but no specific in vivo binding in dynamic PET/MRI studies.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Multidisciplinary
Melissa Chasse, Anna Pees, Anton Lindberg, Steven H. H. Liang, Neil Vasdev
Summary: Positron emission tomography (PET) is a powerful imaging tool used for drug discovery, clinical diagnosis, and disease monitoring. However, the lack of compatible methods and precursors for radiolabeling with fluorine-18 has limited the development of radiotracers. The radiolabeling of electron-rich (hetero)aromatic rings has been a long-standing challenge in producing PET radiopharmaceuticals. In this personal account, the history and applications of spirocyclic iodonium ylide precursors are discussed for the incorporation of fluorine-18 into complex non-activated (hetero)aromatic rings.
Article
Engineering, Biomedical
Michael Barnes, Daryl John O'Connor, Martin Ebert
Summary: A novel method utilizing the He-3(d,p)He-4 nuclear reaction to produce fluorine-18 for PET scans was theoretically evaluated. The theoretical designs involve utilizing helium-3 beams on deuterated plastic targets backed with oxygen-18 heavy-water or super-heavy-water targets. However, practical challenges such as thermal and target degradation effects make the current systems technically infeasible despite the potential advantages over cyclotron-based production.
PHYSICAL AND ENGINEERING SCIENCES IN MEDICINE
(2021)
Article
Medicine, Research & Experimental
Hongzhang Yang, Lei Zhang, Huanhuan Liu, Yunming Zhang, Zhaobiao Mou, Xueyuan Chen, Jingchao Li, Fengming He, Zijing Li
Summary: 18F-labeled fluorothiophosphate (FTP) synthons with high radiochemical yields can be rapidly generated in reaction solutions using wet [18F]F- without the need for substrate pre-modification or lengthy radiosynthesis procedures. This simplified one-pot 18F-labeling method allows for the visualization and translation of a variety of biomolecules, making it valuable for modern positron emission tomography techniques.
Article
Chemistry, Multidisciplinary
Chris Hoffmann, Niklas Kolks, Daniel Smets, Alexander Haseloer, Benedikt Groener, Elizaveta A. Urusova, Heike Endepols, Felix Neumaier, Uwe Ruschewitz, Axel Klein, Bernd Neumaier, Boris D. Zlatopolskiy
Summary: In this study, a series of complexes were systematically evaluated and several generally applicable mediators were identified for highly efficient radiofluorination. The utilization of these mediators significantly improved the labeling yields, even with lower precursor amounts. The practicality of the novel mediators was demonstrated by the efficient production of five PET tracers and transfer of the method to an automated radiosynthesis module.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Review
Pharmacology & Pharmacy
Chao Wang, Rong Lin, Shaobo Yao
Summary: This review focuses on recent advances in the synthesis, radiolabeling, and application of a series of F-18-labeled amino acid analogs using new F-18-labeling strategies.
Article
Radiology, Nuclear Medicine & Medical Imaging
R. Gallicchio, A. Nardelli, G. Calice, A. Guarini, G. Guglielmi, G. Storto
Summary: This study evaluated the prognostic significance of combined use of FDG and FLT PET/CT in MM patients, showing that PET/CT can predict patient prognosis and that FDG+; FLT- patients have better EFS compared to other groups.
EUROPEAN JOURNAL OF RADIOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Li Wang, Yubai Zhou, Xuedan Wu, Xinrui Ma, Bing Li, Ransheng Ding, Michael A. Stashko, Zhanhong Wu, Xiaodong Wang, Zibo Li
Summary: MerTK is abnormally expressed in various cancers, but the sensitivity of tumors to MerTK suppression may vary. In this study, a radiolabeled agent [F-18]-MerTK-6 was developed and showed prominent uptake in tumors in initial evaluation, suggesting it as a promising PET agent for MerTK imaging.
Review
Biochemistry & Molecular Biology
Felix Francis, Frank Wuest
Summary: Positron emission tomography (PET) is a vital imaging technique used for studying biological and physiological processes, with fluorine-18 (F-18) being a commonly used positron emitter in PET imaging. The presence of fluorine atoms in many drugs opens up possibilities for developing radioligands labeled with fluorine-18.
Review
Chemistry, Organic
Zhu Yuan, Chen Leyuan, Hou Wenbin, Li Yiliang
Summary: Fluorine-18 is widely used in positron emission tomography radiopharmaceuticals, with nucleophilic F-18 fluoride being a common labeling reagent. Fluorine substitution can impact pharmacokinetic parameters, and arenes and heteroarenes are commonly used candidates for F-18 labeling.
CHINESE JOURNAL OF ORGANIC CHEMISTRY
(2021)
Editorial Material
Radiology, Nuclear Medicine & Medical Imaging
Kenji Ishibashi, Masashi Kameyama, Yoshiharu Miura, Jun Toyohara, Kenji Ishii
Summary: F-18-THK5351 PET imaging clearly identifies lesions of astrogliosis in patients with neurological disorders, whereas C-11-L-deprenyl images are noisy and less accurate in comparison.
CLINICAL NUCLEAR MEDICINE
(2021)
Article
Radiology, Nuclear Medicine & Medical Imaging
Yongxiang Tang, Ling Xiao, Chijun Deng, Haoyue Zhu, Xiaomei Gao, Jian Li, Zhiquan Yang, Dingyang Liu, Li Feng, Shuo Hu
Summary: This study investigated the patterns of metabolic abnormalities using [F-18]FDG PET in MTLE patients with different pathologic types. It was found that MTLE patients with isolated gliosis had the worst prognosis and exhibited significant hypometabolism in the insula. Therefore, hypometabolic regions should be prioritized for presurgical evaluation of MTLE patients rather than focusing solely on metabolic uptake values.
EUROPEAN RADIOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Gausiha Rathitharan, Jennifer Truong, Junchao Tong, Tina McCluskey, Jeffrey H. Meyer, Romina Mizrahi, Jerry Warsh, Pablo Rusjan, James L. Kennedy, Sylvain Houle, Stephen J. Kish, Isabelle Boileau
Summary: Research on the brains of chronic MA users suggests that while there is activation of microglial cells, there is no significant increase in microgliosis. This indicates that microglia may not be a substantial therapeutic target for MA addiction, despite their involvement in MA-seeking behavior.
Article
Psychiatry
Nathan J. Kolla, Isabelle Boileau, Karolina Karas, Jeremy J. Watts, Pablo Rusjan, Sylvain Houle, Romina Mizrahi
Summary: Individuals with ASPD have lower FAAH density in the amygdala, while FAAH expression in the cerebellum and striatum is inversely related to impulsivity. Cerebellar FAAH density is also negatively associated with assaultive aggression.
TRANSLATIONAL PSYCHIATRY
(2021)
Article
Neurosciences
Marion Criaud, Jin-Hee Kim, Mateusz Zurowski, Nancy Lobaugh, Sofia Chavez, Sylvain Houle, Antonio P. Strafella
Summary: The study found that anxiety symptoms in Parkinson's disease patients are associated with over-activation of the amygdala and impaired inter-relationship among regions involved in behavior and motor control.
Article
Cardiac & Cardiovascular Systems
H. Smailovic, B. Wilk, G. Wisenberg, J. Sykes, J. Butler, J. Hicks, J. D. Thiessen, F. S. Prato
Summary: The study found that using heparin to suppress myocardial uptake of [F-18]FDG did not alter the determination of myocardial ECV, and the choice of infusion protocol also had no effect on the calculated ECV.
JOURNAL OF NUCLEAR CARDIOLOGY
(2022)
Article
Radiology, Nuclear Medicine & Medical Imaging
Lucas Narciso, Tracy Ssali, Linshan Liu, Heather Biernaski, John Butler, Laura Morrison, Jennifer Hadway, Jeffrey Corsaut, Justin W. Hicks, Michael C. Langham, Felix W. Wehrli, Hidehiro Iida, Keith St Lawrence
Summary: A noninvasive PET/MRI technique for imaging cerebral metabolic rate of oxygen (CMRO2) was proposed and validated in an animal study. The technique uses functional MRI to calibrate PET data, potentially reducing the complexity of PET imaging. The results showed good agreement between regional CMRO2 measurements from the new technique and traditional PET-alone measurements.
JOURNAL OF NUCLEAR MEDICINE
(2021)
Article
Neurosciences
Duncan G. J. Green, Jinhee Kim, Stephen J. Kish, Rachel F. Tyndale, Matthew N. Hill, Antonio P. Strafella, Junchao Tong, Tina McCluskey, Duncan J. Westwood, Sylvain Houle, Nancy J. Lobaugh, Isabelle Boileau
Summary: This study revealed a negative correlation between levels of the endocannabinoid enzyme fatty acid amide hydrolase (FAAH) in the amygdala and functional connectivity in frontoamygdalar circuits involved in stress and affect control. The findings provide preliminary evidence supporting the role of FAAH in regulating brain circuits underlying fear and emotion processing in humans.
JOURNAL OF PSYCHIATRY & NEUROSCIENCE
(2021)
Correction
Neurosciences
J. Kolla Nathan, R. Mizrahi, K. Karas, C. Wang, R. M. Bagby, S. McMain, A. I. Simpson, P. M. Rusjan, R. Tyndale, S. Houle, I. Boileau
Summary: The correction to this paper has been published.
NEUROPSYCHOPHARMACOLOGY
(2021)
Article
Multidisciplinary Sciences
Patricia Di Ciano, Harriet de Wit, Esmaeil Mansouri, Sylvain Houle, Isabelle Boileau, Bernard Le Foll
Summary: PET imaging with [C-11]-(+)-PHNO was used to measure changes in dopamine levels in regions of interest in smokers who had maintained abstinence for 7-10 days. Results showed that smoking cues did not increase craving, and there were no significant changes in dopamine binding potential in most regions except for a decrease in the substantia nigra. Further research with a larger sample size is needed to validate these preliminary findings.
SCIENTIFIC REPORTS
(2021)
Article
Psychiatry
Sophia Attwells, Elaine Setiawan, Pablo M. Rusjan, Cynthia Xu, Stephen J. Kish, Neil Vasdev, Sylvain Houle, Apitharani Santhirakumar, Jeffrey H. Meyer
Summary: Oral minocycline did not significantly reduce TSPO V-T in TRD patients, suggesting that this dosage may be insufficient for reducing gliosis in this condition. Alternative therapeutic approaches or intravenous formulations of minocycline should be considered for targeting gliosis in TRD. Additionally, it should not be assumed that oral minocycline will reduce TSPO V-T or gliosis in humans without empirical evidence.
TRANSLATIONAL PSYCHIATRY
(2021)
Article
Clinical Neurology
Talwinder Gill, Sarah E. Watling, J. Don Richardson, Tina McCluskey, Junchao Tong, Jeffrey H. Meyer, Jerry Warsh, Rakesh Jetly, Michael G. Hutchison, Shawn G. Rhind, Sylvain Houle, Neil Vasdev, Stephen J. Kish, Isabelle Boileau
Summary: Posttraumatic stress disorder (PTSD) may be associated with astrocyte pathology and a decrease in MAO-B levels. Preliminary results suggest a potential reduction in [C-11]SL25.1188 availability in PTSD patients, especially those with comorbid major depressive disorder (MDD). These findings are partly consistent with preclinical studies and recent PET observations, but further replication in a larger PTSD cohort is needed.
EUROPEAN NEUROPSYCHOPHARMACOLOGY
(2022)
Article
Neuroimaging
Tracy Ssali, Lucas Narciso, Justin Hicks, Linshan Liu, Sarah Jesso, Lauryn Richardson, Matthias Gunther, Simon Konstandin, Klaus Eickel, Frank Prato, Udunna C. Anazodo, Elizabeth Finger, Keith St Lawrence
Summary: This study evaluated the similarity between ASL and PET in diagnosing FTD, and the results showed that ASL has the potential to be a cost-effective alternative.
NEUROIMAGE-CLINICAL
(2022)
Article
Chemistry, Inorganic & Nuclear
Farah Kamar, Michael S. Kovacs, Justin W. Hicks
Summary: This study developed and validated an Arduino-based device for purifying [N-13]NH3, aiming to address the increased production costs caused by stricter regulatory oversight. The results showed that the automated method could produce equivalent quality radiopharmaceutical as the manual method, with better reproducibility and robustness.
APPLIED RADIATION AND ISOTOPES
(2022)
Article
Clinical Neurology
Anna Vasilevskaya, Foad Taghdiri, Namita Multani, Miracle Ozzoude, Apameh Tarazi, Mozhgan Khodadadi, Richard Wennberg, Pablo Rusjan, Sylvain Houle, Robin Green, Brenda Colella, Kaj Blennow, Henrik Zetterberg, Thomas Karikari, David Mikulis, Lili-Naz Hazrati, Gabor G. Kovacs, Karen Deborah Davis, Charles Tator, Maria Carmela Tartaglia
Summary: This study investigated the use of plasma pTau181 as a non-invasive measure to assess the risk of neurodegenerative diseases in retired athletes. The results showed that retired athletes had higher levels of plasma pTau181 and its levels were associated with abnormalities in certain brain regions. However, baseline pTau181 levels were not predictive of longitudinal changes in brain volumes or white-matter integrity in the athletes.
JOURNAL OF NEUROLOGY
(2022)
Article
Neurosciences
Jeremy J. Watts, Elisa Guma, Sofia Chavez, Rachel F. Tyndale, Ruth A. Ross, Sylvain Houle, Alan A. Wilson, Mallar Chakravarty, Pablo M. Rusjan, Romina Mizrahi
Summary: Dysregulation of hippocampus neurotransmission and volume has been associated with psychiatric disorders, and anandamide and FAAH are related to normal hippocampus function.
NEUROPSYCHOPHARMACOLOGY
(2022)
Article
Psychiatry
Sarah E. Watling, Samantha Jagasar, Tina McCluskey, Jerry Warsh, Shawn G. Rhind, Peter Truong, Sofia Chavez, Sylvain Houle, Junchao Tong, Stephen J. Kish, Isabelle Boileau
Summary: Preliminary data suggests that chronic methamphetamine (MA) use may cause oxidative stress and inflammation in the brain. This study aimed to investigate the levels of the antioxidant glutathione (GSH) in the brains of chronic MA users and explore the relationship between peripheral immunoinflammatory biomarkers and brain GSH concentrations. The results showed that GSH levels did not differ between MA users and healthy controls, but several immunoinflammatory biomarkers were significantly elevated in MA users and correlated with brain GSH levels.
FRONTIERS IN PSYCHIATRY
(2023)
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
