Article
Chemistry, Inorganic & Nuclear
Sara Cesarec, Fraser Edgar, Titan Lai, Christophe Plisson, Andrew J. P. White, Philip W. Miller
Summary: A novel radiolabelling method using C-11-dithiocarbamate ligands has been developed to generate C-11-labelled Au(i), Au(iii), Pd(ii), and Pt(ii) complexes with high radiochemical yields (71-99%). These labelled complexes were prepared rapidly via a one-pot reaction between C-11-dithiocarbamate ligands and appropriate transition metal chloride precursors.
DALTON TRANSACTIONS
(2022)
Article
Chemistry, Multidisciplinary
Melodie Ferrat, Kenneth Dahl, Magnus Schou
Summary: The preparation of electrophilic C-11-labelled aroyl dimethylaminopyridinium salts through carbonylative cross-coupling provides valuable intermediates for synthesizing primary [C-11]benzamides. This method yields benzamide model compounds, including PARP inhibitors, with moderate to excellent radiochemical yields, paving the way for potential application in PET tracer synthesis.
CHEMISTRY-A EUROPEAN JOURNAL
(2021)
Article
Biochemical Research Methods
Olga Ovdiichuk, Hemantha Mallapura, Florian Pineda, Virginie Hourtane, Bengt Langstrom, Christer Halldin, Sangram Nag, Fatiha Maskali, Gilles Karcher, Charlotte Collet
Summary: The iMiDEV(TM) microfluidic system is a new automated tool for small-scale production of radiopharmaceuticals, utilizing microfluidic cassettes for liquid phase reactions. The system allows for fully automated [F-18]NaF radiosynthesis with an intuitive user interface.
Article
Biochemistry & Molecular Biology
Isaac M. Jackson, E. William Webb, Peter J. H. Scott, Michelle L. James
Summary: This article discusses the importance of PET technology and its applications in studying the central nervous system. It also highlights the challenges and limitations in developing CNS PET tracers. Additionally, it explores the potential applications and impact of computational methods in the design of CNS radiotracers.
ACS CHEMICAL NEUROSCIENCE
(2022)
Review
Biochemistry & Molecular Biology
Anna Pees, Melissa Chasse, Anton Lindberg, Neil Vasdev
Summary: Positron emission tomography (PET) is a molecular imaging technique that uses radiolabelled molecules for in vivo evaluation. Carbon-11 is frequently used for labelling PET tracers, and its short half-life allows for multiple scans in the same subject on the same day. However, its use is limited to facilities with an on-site cyclotron. This review presents new carbon-11 building blocks, radiochemical transformations, and PET tracers that have advanced to first-in-human studies in the past five years.
Review
Chemistry, Inorganic & Nuclear
Sebastien Schmitt, Emmanuel Moreau
Summary: This article reviews all the radiolabeling conditions with chelators used since 2009, aiming to determine the most efficient conditions for the rapid development of future radiotracers. Additionally, it focuses on the limitations of this strategy, particularly in terms of automation.
COORDINATION CHEMISTRY REVIEWS
(2023)
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
Chemistry, Multidisciplinary
Rachael Fay, Jason P. Holland
Summary: This study reports the synthesis of metal ion binding chelates derivatised with tetrazoles for photoradiochemical labelling of monoclonal antibodies. Tetrazoles with extended aromatic systems and auxochromic substituents were studied for tuning excitation towards longer wavelengths. Two photoactivatable chelates were functionalised with tetrazoles for protein labelling with Zr-89, Cu-64, and Ga-68 radionuclides, showing stable radiotracer properties in vitro with high immunoreactivity. Positron emission tomography imaging and biodistribution studies demonstrated the feasibility of tetrazole-based photochemistry for the light-induced synthesis of PET radiotracers.
CHEMISTRY-A EUROPEAN JOURNAL
(2021)
Article
Radiology, Nuclear Medicine & Medical Imaging
Ivan Ho Shon, Thomas Hennessy, Jennifer Guille, Michael P. Gotsbacher, Angelina J. Lay, Bruce McBride, Rachel Codd, Philip J. Hogg
Summary: This study evaluates the biodistribution, radiation dosimetry, safety, and tumor uptake of the novel radiopharmaceutical GA-68 ([GA-68] GA-CDI) for imaging multiple forms of cell death. The results demonstrate that GA-68 ([GA-68] GA-CDI) is safe, has low radiation dosimetry, and excellent biodistribution and imaging characteristics. It shows potential advantages over previous radiopharmaceuticals for imaging cell death and has progressed to a proof-of-concept trial.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2022)
Article
Biochemistry & Molecular Biology
Mateusz Pegier, Krzysztof Kilian, Krystyna Pyrzynska
Summary: Searching for new compounds and synthetic routes for medical applications is a challenge in modern chemistry. Porphyrins can tightly bind metal ions and serve as complexing and delivering agents. Two methods, one using a reducing agent and another utilizing microwave-assisted synthesis, were developed to optimize the reaction of copper ions with water-soluble porphyrins. The proposed methods were successfully applied for radiolabeling of porphyrins with Cu-64.
Article
Pharmacology & Pharmacy
Ibolya Kalman-Szabo, Szilvia Bunda, Norbert Lihi, Zsofia Szaniszlo, Dezso Szikra, Judit Szabo Peline, Aniko Fekete, Barbara Gyuricza, Daniel Szucs, Gabor Papp, Gyorgy Trencsenyi, Ferenc K. Kalman
Summary: Malignant melanoma is a significant public health issue with high metastatic potential, and the early detection using imaging techniques is crucial for long-term survival. The radio-labelled alpha-MSH analog NAPamide has been found to be a suitable diagnostic tool for melanoma detection. In this study, a new radiotracer, [61Cu]Cu-KFTGNAPamide, has been synthesized to take advantage of the positron emitter 61Cu and the melanoma specificity of NAPamide. The [61Cu]Cu-KFTG-NAPamide demonstrated excellent diagnostic features for B16-F10 melanoma tumors through PET imaging.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Chemistry, Multidisciplinary
Tanpreet Kaur, Allen F. Brooks, Katherine M. Liddell, Bradford D. Henderson, Brian G. Hockley, Nocolaas Bohnen, Roger L. Albin, Peter J. H. Scott
Summary: This study reports the development of a fully automated synthesis method for a radiotracer that can monitor MC-I activity in Parkinson's disease and other neurodegenerative diseases. The synthesis achieved a high radiochemical yield, excellent radiochemical purity, and high molar activity.
FRONTIERS IN CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Jimmy E. Jakobsson, Sanjay Telu, Shuiyu Lu, Susovan Jana, Victor W. Pike
Summary: A rapid and high-yield method for synthesizing unsymmetrical acyclic [C-11]ureas using no-carrier-added [C-11]carbonyl difluoride is described. The methodology is compatible with diverse functionality in the substrate amines and produces negligible amounts of unwanted symmetrical [C-11]urea byproducts.
CHEMISTRY-A EUROPEAN JOURNAL
(2021)
Review
Chemistry, Medicinal
Ute Hennrich, Matthias Eder
Summary: Radiotracers targeting prostate-specific membrane antigen (PSMA) are commonly used for PET imaging of prostate cancer, with the recent approval of [Ga-68]Ga-PSMA-11 by the FDA in 2020. This radiopharmaceutical combines a peptidomimetic compound with the radionuclide Ga-68, allowing specific imaging of PSMA-positive tumor cells and potential applications in therapy planning and treatment response evaluation.
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
Biochemistry & Molecular Biology
Lindsey R. Drake, Peter J. H. Scott
ACS CHEMICAL NEUROSCIENCE
(2018)
Article
Biochemical Research Methods
Andrew V. Mossine, Allen F. Brooks, Vadim Bernard-Gauthier, Justin J. Bailey, Naoko Ichiishi, Ralf Schirrmacher, Melanie S. Sanford, Peter J. H. Scott
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
(2018)
Article
Chemistry, Multidisciplinary
So Jeong Lee, Katarina J. Makaravage, Allen F. Brooks, Peter J. H. Scott, Melanie S. Sanford
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2019)
Editorial Material
Biochemistry & Molecular Biology
Vidya Narayanaswami, Lindsey R. Drake, Allen F. Brooks, Jeffrey H. Meyer, Sylvain Houle, Michael R. Kilbourn, Peter J. H. Scott, Neil Vasdev
ACS CHEMICAL NEUROSCIENCE
(2019)
Article
Biochemistry & Molecular Biology
Justin J. Bailey, Lena Kaiser, Simon Lindner, Melinda Wuest, Alexander Thiel, Jean-Paul Soucy, Pedro Rosa-Neto, Peter J. H. Scott, Marcus Unterrainer, David R. Kaplan, Carmen Waengler, Bjoern Waengler, Peter Bartenstein, Vadim Bernard-Gauthier, Ralf Schirrmachert
ACS CHEMICAL NEUROSCIENCE
(2019)
Article
Biochemistry & Molecular Biology
Lindsey R. Drake, Jonathan M. Pham, Timothy J. Desmond, Andrew Mossine, So Jeong Lee, Michael R. Kilbourn, Robert A. Koeppe, Allen F. Brooks, Peter J. H. Scott
ACS CHEMICAL NEUROSCIENCE
(2019)
Article
Chemistry, Medicinal
Vadim Bernard-Gauthier, Andrew V. Mossine, Ashley Knight, Debasis Patnaik, Wen-Ning Zhao, Chialin Cheng, Hema S. Krishnan, Lucius L. Xuan, Peter S. Chindavong, Surya A. Reis, Jinshan Michael Chen, Xia Shao, Jenelle Stauff, Janna Arteaga, Phillip Sherman, Nicolas Salem, David Bonsall, Brenda Amaral, Cassis Varlow, Lisa Wells, Laurent Martarello, Shil Patel, Steven H. Liang, Ravi G. Kurumbail, Stephen J. Haggarty, Peter J. H. Scott, Neil Vasdev
JOURNAL OF MEDICINAL CHEMISTRY
(2019)
Editorial Material
Biochemistry & Molecular Biology
Jean Jacques Vanden Eynde, Arduino A. Mangoni, Jarkko Rautio, Jerome Leprince, Yasu-Taka Azuma, Alfonso T. Garcia-Sosa, Christopher Hulme, Josef Jampilek, Rafik Karaman, Wei Li, Paula A. C. Gomes, Dimitra Hadjipavlou-Litina, Raffaele Capasso, Athina Geronikaki, Laura Cerchia, Jean-Marc Sabatier, Rino Ragno, Tiziano Tuccinardi, Andrea Trabocchi, Jean-Yves Winum, F. Javier Luque, Katalin Prokai-Tatrai, Mariana Spetea, Michael Guetschow, Ivan Kosalec, Catherine Guillou, M. Helena Vasconcelos, George Kokotos, Giulio Rastelli, Maria Emilia de Sousa, Clementina Manera, Sandra Gemma, Stefano Mangani, Carlo Siciliano, Stefania Galdiero, Hong Liu, Peter J. H. Scott, Cristobal de los Rios, Luigi A. Agrofoglio, Simona Collina, Rita C. Guedes, Diego Munoz-Torrero
Article
Biochemistry & Molecular Biology
Peter J. H. Scott, Robert A. Koeppe, Xia Shao, Melissa E. Rodnick, Alexandra R. Sowa, Bradford D. Henderson, Jenelle Stauff, Phillip S. Sherman, Janna Arteaga, Dennis J. Carlo, Ronald B. Moss
Editorial Material
Biochemistry & Molecular Biology
Michael Guetschow, Jean Jacques Vanden Eynde, Josef Jampilek, CongBao Kang, Arduino A. Mangoni, Paola Fossa, Rafik Karaman, Andrea Trabocchi, Peter J. H. Scott, Johannes Reynisson, Simona Rapposelli, Stefania Galdiero, Jean-Yves Winum, Chiara Brullo, Katalin Prokai-Tatrai, Arun K. Sharma, Matthieu Schapira, Yasu-Taka Azuma, Laura Cerchia, Mariana Spetea, Giangiacomo Torri, Simona Collina, Athina Geronikaki, Alfonso T. Garcia-Sosa, M. Helena Vasconcelos, Maria Emilia Sousa, Ivan Kosalec, Tiziano Tuccinardi, Iola F. Duarte, Jorge A. R. Salvador, Massimo Bertinaria, Maurizio Pellecchia, Jussara Amato, Giulio Rastelli, Paula A. C. Gomes, Rita C. Guedes, Jean-Marc Sabatier, Ana Estevez-Braun, Bruno Pagano, Stefano Mangani, Rino Ragno, George Kokotos, Margherita Brindisi, Florenci V. Gonzalez, Fernanda Borges, Mariarosaria Miloso, Jarkko Rautio, Diego Munoz-Torrero
Article
Chemistry, Organic
Andrew V. Mossine, Sean S. Tanzey, Allen F. Brooks, Katarina J. Makaravage, Naoko Ichiishi, Jason M. Miller, Bradford D. Henderson, Marc B. Skaddan, Melanie S. Sanford, Peter J. H. Scott
ORGANIC & BIOMOLECULAR CHEMISTRY
(2019)
Article
Chemistry, Multidisciplinary
Stefan Verhoog, Allen F. Brooks, Wade P. Winton, Benjamin L. Viglianti, Melanie S. Sanford, Peter J. H. Scott
CHEMICAL COMMUNICATIONS
(2019)
Article
Biochemical Research Methods
Taylor J. Forrest, Timothy J. Desmond, Mohamad Issa, Peter J. H. Scott, Gregory J. Basura
Review
Chemistry, Medicinal
Ralf Schirrmacher, Justin J. Bailey, Andrew V. Mossine, Peter J. H. Scott, Lena Kaiser, Peter Bartenstein, Simon Lindner, David R. Kaplan, Alexey Kostikov, Gert Fricker, Anne Mahringer, Pedro Rosa-Neto, Esther Schirrmacher, Carmen Waengler, Bjoern Waengler, Alexander Thiel, Jean-Paul Soucy, Vadim Bernard-Gauthier
Article
Chemistry, Multidisciplinary
So Jeong Lee, Allen F. Brooks, Naoko Ichiishi, Katarina J. Makaravage, Andrew Mossine, Melanie S. Sanford, Peter J. H. Scott
CHEMICAL COMMUNICATIONS
(2019)