Review
Chemistry, Multidisciplinary
Ya-Qiong Yan, Hao Wang, Yuliang Zhao
Summary: Radionuclide imaging is a premier imaging method in clinical practice, utilizing PET and SPECT to detect anatomical abnormalities. Peptides as targeting vectors for contrast agents offer high specificity and low toxicity. Radiolabeled peptide probes have become essential tools for clinical radionuclide diagnosis.
CHINESE CHEMICAL LETTERS
(2022)
Review
Chemistry, Multidisciplinary
Giordana Salvi de Souza, Dimitri B. A. Mantovani, Pascalle Mossel, Bartholomeus C. M. Haarman, Ana Maria Marques da Silva, Hendrikus H. Boersma, Cristiane R. G. Furini, Adriaan A. Lammertsma, Charalampos Tsoumpas, Gert Luurtsema
Summary: The oral route is widely used and preferred for drug administration. Accurate quantification of drug absorption, distribution, metabolism, excretion, and characterization is crucial for drug development. In vivo methods such as gamma-scintigraphy, MRI, and PET have been used to analyze gastrointestinal absorption. This review focuses on PET studies using oral tracers, revealing variations in acquisition protocols, quantification methods, and pharmacokinetic parameters. Human studies showed 10-30 minutes for tracer to reach the intestine and about 100 minutes to reach peak concentration in the brain. Rodent studies estimated different pharmacokinetic parameters, indicating PET's potential for non-invasive measurement of drug absorption and distribution. Long Axial Field of View (LAFOV) PET scanners can reduce administered dose, making oral administration feasible for clinical studies.
JOURNAL OF CONTROLLED RELEASE
(2023)
Review
Oncology
Yuan Huang, Junying Fan, Yi Li, Shaozhi Fu, Yue Chen, Jingbo Wu
Summary: The hypoxic state in solid tumors can lead to resistance to therapy and poor prognosis factors like metastasis and recurrence. Accurate quantification, mapping, and monitoring of hypoxia, as well as targeted therapy, are crucial for improving patient survival. PET imaging remains the most widely used method for evaluating tumor hypoxia, but further research is needed to improve methods for detecting tumor hypoxia.
FRONTIERS IN ONCOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Pejman Shahrokhi, Arezou Masteri Farahani, Mohammad Tamaddondar, Farzaneh Rezazadeh
Summary: PSMA, a glycosylated protein expressed in prostatic tissue, is also overexpressed in endothelial cells of non-prostate diseases. The use of small molecules targeting PSMA for imaging has shown improved diagnostic sensitivity and specificity for various malignancies, impacting patient management.
CHEMICAL BIOLOGY & DRUG DESIGN
(2022)
Review
Immunology
Jeffrey M. A. van der Krogt, Wouter H. van Binsbergen, Conny J. van der Laken, Sander W. Tas
Summary: PET is a nuclear imaging technique that can visualize immunological targets in rheumatoid arthritis (RA) and monitor therapeutic effects and stratify the immune phenotype. Novel PET tracers can specifically visualize cells and processes related to pathology, with important applications in RA diagnosis and prediction of treatment outcomes.
AUTOIMMUNITY REVIEWS
(2021)
Review
Radiology, Nuclear Medicine & Medical Imaging
Valeria Romeo, Thomas H. Helbich, Katja Pinker
Summary: The recent introduction of hybrid positron emission tomography/magnetic resonance imaging (PET/MRI) as a promising imaging modality for breast cancer assessment has sparked extensive research on its clinical applications. This state-of-the-art review provides an overview of advanced MRI techniques, PET tracers, and the use of radiomics and artificial intelligence techniques in hybrid breast PET/MRI. The strengths and limitations of hybrid PET/MRI in the real world are also discussed.
JOURNAL OF MAGNETIC RESONANCE IMAGING
(2023)
Review
Chemistry, Multidisciplinary
Xueqian Chen, Wenchao Niu, Zhongying Du, Yong Zhang, Dongdong Su, Xueyun Gao
Summary: This review discusses the applications of Cu-64 labeled nanomaterials in biomedicine, including PET imaging, pharmacokinetic monitoring, and imaging guided therapy. It emphasizes the importance of appropriate carrier characteristics and radiolabeling strategies in Cu-64 PET imaging.
CHINESE CHEMICAL LETTERS
(2022)
Review
Biochemistry & Molecular Biology
Zohreh Mohammadi, Hadi Alizadeh, Janos Marton, Paul Cumming
Summary: Hyperphosphorylated tau aggregates are characteristic features of Alzheimer's disease (AD). The development of molecular imaging of tau by positron emission tomography (PET) started with [F-18]FDDNP, which had off-target binding to tau and obtained regional specificity through the distribution of amyloid beta and tau in AD brains. Several tau PET tracers have been developed, with F-18-flortaucipir being the first approved by the FDA. These tracers differ in selectivity, off-target binding, and uptake in white matter. In this review, the binding properties of the tracers in vitro and their effectiveness in discriminating between AD patients and healthy controls were compared. The available tracers showed good discrimination, with higher effectiveness in more severe AD patients.
Article
Biochemistry & Molecular Biology
Yafeng Wang, Menglin Xue, Ruixuan Gao, Soumyadeep Chakraborty, Shaohui Wang, Xue Zhao, Meng Gu, Chuanhai Cao, Xingmin Sun, Jianfeng Cai
Summary: Antibiotic resistance is a major global health issue and there is a pressing need for the development of new antibiotics to combat drug resistance. In this article, the design of lipidated dendrimeric ?-AApeptides as a new class of antimicrobial agents is reported. These AApeptides showed potent and broad-spectrum activity against both Gram-positive and Gram-negative bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). Mechanistic studies revealed that the dendrimeric AApeptides rapidly kill bacteria by permeabilizing bacterial membranes, similar to host-defense peptides (HDPs). These dendrimers also have a low likelihood of inducing antibiotic resistance. The easy synthesis and strong antimicrobial activity make these lipidated dendrimeric ?-AApeptides a new generation of antibacterial agents.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Clinical Neurology
Steven Y. Yap, Barbara Frias, Melissa C. Wren, Michael Scholl, Nick C. Fox, Erik Arstad, Tammaryn Lashley, Kerstin Sander
Summary: A new generation of tau PET tracers has been developed for the imaging of Alzheimer's disease and other dementias with high specificity, showing potential to differentiate Alzheimer's disease from other dementias in clinical applications. Despite some remaining challenges, these new tracers have the potential to play an important role in clinical practice.
Article
Chemistry, Organic
Manuele Musolino, Ian N. Fleming, Lutz F. Schweiger, David O'Hagan, Sergio Dall'Angelo, Matteo Zanda
Summary: The synthesis of five radiotracers with different oxyamine spacers between the hypoxia-reactive 2-nitroimidazole moiety and the 5-[F-18]-fluorodeoxyribose prosthetic group was reported. Among them, tracer 15 d displayed superior uptake kinetics and similar selectivity for hypoxic cells compared to standard hypoxia tracers. Lipophilicity and structural rigidity significantly influenced the selectivity of the tracers towards hypoxic cells.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Medicine, Research & Experimental
Wei Zheng, Xuebo Cheng, Hualong Chen, Zeng Jiang, Yuli Sun, Ziyue Yu, Tingyu Yang, Lu Zhang, Yajing Liu, Xunming Ji, Zehui Wu
Summary: The abnormal expression of aromatase is associated with various neurological diseases and tumors. In this study, F-18 and Ga-68 labeled compounds were designed and synthesized to bind to aromatase. Two of these compounds, BIBD-069 and BIBD-071, showed high affinity for aromatase. They were successfully radiolabeled and specifically bound to aromatase in vitro and in vivo. These compounds can serve as important tools for the diagnosis and treatment of aromatase-related diseases.
MOLECULAR PHARMACEUTICS
(2022)
Article
Chemistry, Medicinal
Yingfang He, Matthias Schild, Uwe Grether, Jorg Benz, Lea Leibrock, Dominik Heer, Andreas Topp, Ludovic Collin, Bernd Kuhn, Matthias Wittwer, Claudia Keller, Luca C. Gobbi, Roger Schibli, Linjing Mu
Summary: A novel reversible MAGL inhibitor, (R)-[F-18]13, was successfully synthesized and showed high brain uptake in PET scans in mice. Target occupancy studies revealed its potential as a promising PET probe for visualizing MAGL non-invasively in vivo.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Dingyao Gao, Yinxing Miao, Siqin Ye, Chunmei Lu, Gaochao Lv, Ke Li, Chunjing Yu, Jianguo Lin, Ling Qiu
Summary: GGT is a key biomarker for cancer diagnosis due to its high expression in malignant tumors. A novel PET imaging probe, [F-18]GCPA(2), has been designed for targeted monitoring of GGT expression in living subjects, showing potential for clinical applications.
Review
Chemistry, Medicinal
Ma Su, Yifan Zhu, Wei Wang, Feng Liu, Huanqiu Li
Summary: γ-AApeptides, a new class of peptidomimetics based on peptide nucleic acids (PNAs) backbone, have advantages such as resistance to degradation, enhanced chemodiversity, good selectivity, and outstanding bioactivity, making them promising candidates for drug development and molecular probe applications. Their development has been driven by structure-based design, combinatorial library screening, and peptides selfassembly and folding, leading to applications in a variety of fields including antibiotic and antiviral agents, nanomaterials, and supramolecular structures.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Tyler A. Bailey, Veronika Mocko, Katherine M. Shield, Dahlia D. An, Andrew C. Akin, Eva R. Birnbaum, Mark Brugh, Jason C. Cooley, Jonathan W. Engle, Michael E. Fassbender, Stacey S. Gauny, Andrew L. Lakes, Francois M. Nortier, Ellen M. O'Brien, Sara L. Thiemann, Frankie D. White, Christiaan Vermeulen, Stosh A. Kozimor, Rebecca J. Abergel
Summary: The development of targeted alpha therapies can potentially revolutionize disease treatment by delivering destructive radiation to diseased cells while sparing healthy tissue. Despite challenges with incompatible isotopes, researchers successfully produced Ce-134 for PET imaging, demonstrating its potential as a candidate for imaging Ac-225 or Th-227. Rigorous control of the Ce-III/Ce-IV redox couple was crucial for success in these experiments.
Article
Chemistry, Multidisciplinary
Pu Duan, Kelly J. Chen, Gayani Wijegunawardena, Aurelio J. Dregni, Harrison K. Wang, Haifan Wu, Mei Hong
Summary: This study investigates the binding sites of a PET ligand, flutemetamol, to the 40-residue Alzheimer's beta-amyloid peptide (A beta 40) using F-19 and C-13 solid-state NMR. The results show that flutemetamol binds tightly to half of the peptides in the A beta 40 fibril polymorph and loosely to the other half. The study also reveals that specific segments in the peptide form multiple binding sites, and the ligand orientations and positions at these sites are consistent across different A beta polymorphs. These findings provide insights into the structural basis for the specificity of different PET tracers to different amyloid proteins.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2022)
Review
Pharmacology & Pharmacy
Kaelyn V. Becker, Margarita Chernysheva, Todd E. Barnhart, Katherine Gagnon, Jonathan W. Engle
Summary: This review explores gallium-68 production strategies including accelerator target designs at various beam energies and intensities, as well as radiochemical separation techniques for isolating Ga-68. It also discusses the recovery of isotopically enriched target material from irradiated targets and the implications of these techniques for downstream radiolabeling applications.
CURRENT RADIOPHARMACEUTICALS
(2021)
Article
Chemistry, Inorganic & Nuclear
C. J. Kutyreff, T. E. Barnhart, Y. H. Lo, S. Happel, R. J. Nickles, P. A. Ellison, E. Aluicio-Sarduy, J. W. Engle
Summary: This study reports a novel intermetallic target of Co and Ga for accelerator production of no-carrier-added Ge-69/71, as well as a new method to isolate Ge with high yields and purities, which will further promote the development of targeted radionuclide therapy.
APPLIED RADIATION AND ISOTOPES
(2022)
Article
Chemistry, Analytical
Francis Berthias, Hayden A. Thurman, Gayani Wijegunawardena, Haifan Wu, Alexandre A. Shvartsburg, Ole N. Jensen
Summary: Advances in proteomics have shown the ubiquity and biological importance of diverse proteoforms. The ability to separate and analyze intact isomeric proteoforms is crucial for understanding their functions. A novel technique using trapped IMS was demonstrated to achieve baseline resolution of isomeric proteoforms, opening new avenues in proteomics and epigenetics.
ANALYTICAL CHEMISTRY
(2022)
Article
Chemistry, Analytical
Xin Shu, Qing-Qing Liao, Shang-Tong Li, Lu Liu, Xiajun Zhang, Lianqi Zhou, Long Zhang, Irene Coin, Lei Wang, Haifan Wu, Bing Yang
Summary: Post-translational modification of proteins by Ubiquitin (Ub) and Ubiquitin-like proteins (Ubls) can be reversed by deconjugating enzymes. Developing cell-permeable Ub/Ubl probes for live cell applications is challenging. Here, genetically encoded cross-linkable Ub/Ubl probes were developed to investigate deconjugating enzyme activity in physiological environments.
ANALYTICAL CHEMISTRY
(2023)
Article
Pharmacology & Pharmacy
Hailey A. Houson, Volkan Tekin, Wilson Lin, Eduardo Aluicio-Sarduy, Jonathan W. Engle, Suzanne E. Lapi
Summary: The study demonstrates that [Co-55] Co-NOTA-NT-20.3 exhibits superior cell uptake and increasing tumor to blood ratios over time compared to [Ga-68] Ga-NOTA-NT-20.3 and [Cu-64] Cu-NOTA-NT-20.3, indicating its enhanced targeting efficacy for NTSR1.
Article
Biochemistry & Molecular Biology
Gayani Wijegunawardena, Erika Castillo, Brandy Henrickson, Regan Davis, Carlo Condello, Haifan Wu
Summary: Mutations in the microglia-associated gene TREM2 increase the risk of Alzheimer's disease. Traditional methods for studying TREM2 rely on recombinant proteins, but achieving site-specific labeling is challenging. In this study, we synthesized the 116 amino acid TREM2 ectodomain chemically and demonstrated its functional effects on microglial cells. We also investigated the importance of glycosylation in TREM2's stability. This method allows for site-specific labeling of TREM2 and further advances our understanding of its role in Alzheimer's disease.
ACS CHEMICAL NEUROSCIENCE
(2023)
Article
Chemistry, Multidisciplinary
Zachary T. Rosenkrans, Jessica C. Hsu, Eduardo Aluicio-Sarduy, Todd E. Barnhart, Jonathan W. Engle, Weibo Cai
Summary: The therapeutic efficacy of photodynamic therapy is limited by the ability of light to penetrate tissues. Cerenkov luminescence from radionuclides has been proposed as an alternative light source in a strategy called Cerenkov radiation-induced therapy. Semiconducting polymer nanoparticles (SPNs) with ideal optical properties can amplify the relatively weak Cerenkov luminescence produced by radionuclides. An optimized photosensitizer-doped SPN was investigated as a nanosystem for cancer theranostics and showed excellent potential in an in vivo tumor therapy study.
ADVANCED FUNCTIONAL MATERIALS
(2023)
Article
Chemistry, Organic
Jason C. Mixdorf, Sabrina L. V. Hoffman, Eduardo Aluicio-Sarduy, Todd E. Barnhart, Jonathan W. Engle, Paul A. Ellison
Summary: A copper-mediated radiobromination method for (hetero)-aryl boronic pinacol esters is presented. Cyclotron-produced [76/77Br]bromide was isolated using an anion exchange cartridge, and the pre-equilibration and elution solutions played a crucial role in downstream deboro-bromination. The bromination reaction showed compatibility with a wide range of functional groups and successfully labeled molecules with varying electronic and steric effects. Biologically active radiopharmaceuticals, including two radio-brominated inhibitors of poly ADP ribose polymerase, were synthesized for targeting ovarian, breast, and prostate cancers.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Margarita N. Kretowicz, Kendall E. Barrett, Todd E. Barnhart, Jonathan W. Engle
Summary: 52gMn is a promising radionuclide for PET, and enriched 52Cr targets are needed to minimize the formation of 54Mn impurities. In this study, recyclable, electroplated 52Cr metal targets were developed, resulting in >99.89% radionuclidically pure 52gMn. The replating efficiency was 60 ± 20%, and unplated chromium was recovered with 94% efficiency.
APPLIED RADIATION AND ISOTOPES
(2023)
Article
Chemistry, Inorganic & Nuclear
Aohan Hu, Kirsten E. Martin, Dariusz Smilowicz, Eduardo Aluicio-Sarduy, Shelbie J. Cingoranelli, Suzanne E. Lapi, Jonathan W. Engle, Eszter Boros, Justin J. Wilson
Summary: This study describes the synthesis of a bifunctional chelator, py-macrodipa-NCS, and its conjugation to a prostate-specific membrane antigen (PSMA)-binding moiety for radiolabeling complex preparation. In vivo experiments using mice showed that the resulting complex effectively delivered the radiometals to PSMA-positive tumor sites, but partial radiometal dissociation was observed, indicating the need for further optimization.
EUROPEAN JOURNAL OF INORGANIC CHEMISTRY
(2023)
Article
Biology
Paul A. Clark, Raghava N. Sriramaneni, Amber M. Bates, Won Jong Jin, Justin C. Jagodinsky, Reinier Hernandez, Trang Le, Justin J. Jeffery, Ian R. Marsh, Joseph J. Grudzinski, Eduardo Aluicio-Sarduy, Todd E. Barnhart, Bryce R. Anderson, Ishan Chakravarty, Ian S. Arthur, KyungMann Kim, Jonathan W. Engle, Bryan P. Bednarz, Jamey P. Weichert, Zachary S. Morris
Summary: The addition of low-dose radiation with ISV administration outside the brain significantly increases survival in animals co-harboring melanoma brain tumors. Timing of whole-brain radiation treatment (WBRT) is critical, with the effect on survival potentially mediated through immune modulation rather than just direct tumor cell cytotoxicity.
RADIATION RESEARCH
(2021)
Article
Chemistry, Multidisciplinary
Pu Duan, Kelly J. Chen, Gayani Wijegunawardena, Aurelio J. Dregni, Harrison K. Wang, Haifan Wu, Mei Hong
Summary: PET imaging is an important method for diagnosing neurodegenerative disorders, with various PET tracers showing different binding capacities and specificities to target proteins. Through NMR studies, the details of flutemetamol binding to Aβ40 were investigated, revealing insights into the interaction and comparison with other amyloid proteins.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2022)
Review
Chemistry, Multidisciplinary
Dan He, Yawen Li, Fuwen Zhao, Yuze Lin
Summary: High trap density in organic solar cells leads to localized charge carriers and reduced carrier lifetime, limiting device efficiency. This feature article summarizes the recent advances of trap suppression by material design and device engineering.
CHEMICAL COMMUNICATIONS
(2024)
Review
Chemistry, Multidisciplinary
Olivier Monfort, Arshitha Madhusudhan, Martin Motola
Summary: This article presents the advantages of coupling photocatalysis and Fenton-based processes for environmental remediation and discusses their synergy. It critically examines the simultaneous triggering of these two processes and provides insights into research approaches. The study aims to enhance understanding of this complex process and highlight the potential integration of new catalysts in current wastewater treatment technology.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Multidisciplinary
Manideepa Dhar, Chittaranjan Mishra, Avijit Das, Uttam Manna
Summary: An approach of 'polymerization of monomers in its aggregated form' has been introduced to tailor the water wettability of fibrous and porous substrates, achieving hydrophobicity to superhydrophobicity transition, as well as patterned wettability. This facile chemical method provides a durable coating with adjustable and patterned wettability for various potential applications.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Multidisciplinary
Saswat Ranjan Bhoi, Chhanda Debnath, Shikha Gandhi
Summary: In this article, a novel catalytic reaction using Pd(0) and Bronsted acid is reported for the synthesis of biologically important imidazolidinone-fused N-heterocycles through redox-neutral intramolecular N-allylation of indoles and pyrroles with alkynes. This atom-economical method is applicable to a wide range of substrates and eliminates the need for leaving groups or oxidizing agents commonly used in traditional allylation reactions.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Multidisciplinary
Longkun Chen, Mingshuai Zhang, Meichen Liu, Zhuoyuan Liu, Yuetong Qiu, Zhilai Zhang, Fuchao Yu, Jiuzhong Huang
Summary: In this study, an efficient Rh(III)-catalyzed selective mono- and dual-C-H bond functionalization/cyclization with iodonium ylide as the sole coupling partner was demonstrated. Fused benzodiazepine skeletons were obtained in excellent yields, providing an improved approach to dual C-H unsymmetrical functionalization.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Multidisciplinary
Alice Kennett, Sven Epple, Gabriella van der Valk, Irene Georgiou, Evelyne Gout, Romain R. Vives, Angela J. Russell
Summary: This study presents the design and synthesis of sulfated disaccharide inhibitors based on IdoA(2S)-GlcNS(6S), which showed potent inhibition of Sulf-2. The results suggest that IdoA(2S)-GlcNS(6S) is the shortest fragment size required for effective inhibition of Sulfs, and a trisulfated disaccharide is identified as the minimal fragment size of heparan sulfate for effective endosulfatase inhibition.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Multidisciplinary
Mauro Garbini, Andrea Brunetti, Riccardo Pedrazzani, Magda Monari, Massimo Marcaccio, Giulio Bertuzzi, Marco Bandini
Summary: The self-adaptability of galvanostatic electrolysis was found to be helpful in a multistage chemo- and diastereoselective electrochemically promoted cyclodimerization of chalcones. Through a series of reductive events, densely functionalized cyclopentanes with five contiguous stereocenters were obtained (25 examples, yields up to 95%, dr values up to >20:1). Further experimental and electrochemical investigations indicated the crucial role of dynamic kinetic resolution of the aldol intermediate in the reaction mechanism.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Multidisciplinary
Dhananjay S. Nipate, Neha Meena, Prakash N. Swami, Krishnan Rangan, Anil Kumar
Summary: In this study, the synthesis of functionalized benzo[a]phenazines and indazolo[2,3-a]quinolines was achieved through Rh(III)-catalyzed oxidative annulation of 2-arylquinoxalines and 2-aryl-2H-indazoles with allyl alcohols. The method showed a wide substrate scope, excellent functional group tolerance, good to high yields of annulated products, and the capability for scaled-up synthesis. A tentative mechanism of the annulation reaction was proposed based on a preliminary mechanistic investigation.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Multidisciplinary
Ruonan Zhang, Abudukadi Tudi, Xia Yang, Xuping Wang, Zhihua Yang, Shujuan Han, Shilie Pan
Summary: A new lead tellurium borate material with a unique fundamental building block [B4O10] was synthesized and found to exhibit high birefringence. The structure-property relationship was discussed using first-principles calculations.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Multidisciplinary
Amresh Kumar Singh, Baishali Thakurta, Anupam Giri, Monalisa Pal
Summary: This study introduces three key concepts for the quick synthesis of large-scale high-quality 2D materials films and their utilization in device fabrication.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Multidisciplinary
Reina Hagiwara, Shun Nishimura, Kosuke Okeyoshi
Summary: A copolymer-conjugated nanocatalytic system has been developed to improve electron transfer and enhance photoinduced H2 generation.
CHEMICAL COMMUNICATIONS
(2024)
