Article
Biochemical Research Methods
Manshu Li, Xinrui Ma, Christopher J. Molnar, Shuli Wang, Zhanhong Wu, Vladimir V. Popik, Zibo Li
Summary: An efficient modular strategy for rapid assembly of PET agents has been developed, which allows for a combinatorial approach to cross-linking of positron emitter-bearing prosthetic groups with various ligands. The strategy utilizes a sequential and selective double-click reaction, specifically the strain-promoted azide alkyne cyclization (SPAAC) coupling, to produce a stable intermediate that can be modified with azide-tagged biomolecules. Several PET agents have been successfully constructed using this strategy, and the modularity of the approach has been demonstrated in the preparation of PSMA PET agents, where the hydrophilicity can be easily modified to improve tumor to background contrast.
BIOCONJUGATE CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Shivashankar Khanapur, Kenneth Lye, Dipendu Mandal, Xin Jie Wee, Edward G. Robins, Rowan D. Young
Summary: We present a general method for labeling both CF3 and CF2H groups in various chemical settings. The method provides good radiochemical yields and molar activities, and is applicable to biologically relevant compounds. The use of target compounds as starting materials and the simplicity of the method make it attractive for drug and radiotracer development.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Chemistry, Multidisciplinary
Josiah J. Newton, Gokce Engudar, Alan J. Brooke, Matthew B. Nodwell, Holly Horngren-Rhodes, Rainer E. Martin, Paul Schaffer, Robert Britton, Chadron M. Friesen
Summary: This article describes a unique and general process for O-H, N-H, and C-H difluoromethylation, involving the formation of a transient dithiole and facile desulfurative fluorination using silver(I) fluoride. The process is compatible with a wide range of functional groups and can be used for fluorine-18 labeling. It is expected to inspire new efforts in medicinal chemistry, agrochemistry, and radiotracer production.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Review
Medicine, Research & Experimental
Julie Bolcaen, Janke Kleynhans, Shankari Nair, Jeroen Verhoeven, Ingeborg Goethals, Mike Sathekge, Charlot Vandevoorde, Thomas Ebenham
Summary: Despite challenges in treating glioblastoma, advancements in radiopharmaceuticals offer potential for individualized treatment options. The development of targeted radionuclide therapy promises personalized approaches based on molecular-level assessments of disease. This development opens new possibilities for tailored therapeutic modalities, although challenges remain in effectively treating glioblastoma.
Article
Chemistry, Organic
Umberto M. Battisti, Marius Mueller, Rocio Garcia-Vazquez, Matthias Manfred Herth
Summary: This study improves the labeling method of tetrazines for pretargeted imaging. The use of basic preconditioning conditions and low basic anions allows successful labeling of bispyridyl and H-tetrazines, with high labeling efficiency.
Article
Radiology, Nuclear Medicine & Medical Imaging
Federica Pisaneschi, Nerissa T. Viola
Summary: This article discusses the validation studies essential for characterizing new radiopharmaceuticals derived from small molecules, peptides or proteins, including the chemistry and radiochemistry metrics to establish the identity of the imaging agent, as well as in vitro and in vivo studies to examine the radiotracer's mechanism of action.
MOLECULAR IMAGING AND BIOLOGY
(2022)
Article
Chemistry, Organic
Chunling Blue Lan, Karine Auclair
Summary: Ammonium chloride facilitates the reaction between amines and potassium cyanate, allowing for rapid and convenient synthesis of monosubstituted ureas. This method is tolerant of various functional groups and compatible with different nucleophiles and protecting groups. The products can precipitate out of solution, eliminating the need for column chromatography.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Avinash H. Bansode, Bhuvanachandra Bhoopal, Krishna Kumar Gollapelli, Naresh Damuka, Ivan Krizan, Mack Miller, Suzanne Craft, Akiva Mintz, Kiran Kumar Solingapuram Sai
Summary: Hyper-phosphorylation of tau proteins leads to impairment and destabilization of neuronal microtubules, which is associated with various neurological disorders such as Alzheimer's disease and Parkinson's disease. Recent scientific evidence suggests that MT-stabilizing agents can protect against neurodegeneration in the treatment of Alzheimer's disease. In this study, a brain-penetrant PET radiopharmaceutical, [C-11]MPC-6827, was developed and its binding constants and metabolic stability were evaluated in vivo.
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)
Editorial Material
Radiology, Nuclear Medicine & Medical Imaging
Matthias M. Herth, Simon Ametamey, Dmitrii Antuganov, Andreas Bauman, Mathias Berndt, Allen F. Brooks, Guy Bormans, Yearn Seong Choe, Nic Gillings, Urs O. Hafeli, Michelle L. James, Klaus Kopka, Vasko Kramer, Raisa Krasikova, Jacob Madsen, Linjing Mu, Bernd Neumaier, Markus Piel, Frank Roesch, Tobias Ross, Roger Schibli, Peter J. H. Scott, Vladimir Shalgunov, Neil Vasdev, Wolfgang Wadsak, Brian M. Zeglis
Summary: Radiochemical conversion is crucial in radiopharmaceutical chemistry, measuring the efficiency of reaction by studying the transformation of components in a crude reaction mixture. On the other hand, radiochemical yield is more suited to determining the efficiency of the entire reaction process, including separation, isolation, filtration, and formulation.
NUCLEAR MEDICINE AND BIOLOGY
(2021)
Article
Chemistry, Multidisciplinary
Angus J. Koller, Shefali Saini, Ivis F. Chaple, M. Andrey Joaqui-Joaqui, Brett M. Paterson, Michelle T. Ma, Philip J. Blower, Valerie C. Pierre, Jerome R. Robinson, Suzanne E. Lapi, Eszter Boros
Summary: This study fills the knowledge gap in stabilizing molecular Ti4+ species in aqueous environments through a thorough thermodynamic screening of bidentate chelators with Ti4+ in aqueous solution, as well as computational and structural analyses of key compounds. Furthermore, the chelation capacity of hexadentate analogues towards the Ti-45 isotope for positron emission tomography (PET) imaging applications was evaluated, showing excellent performance for kit-formulation.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Chemistry, Multidisciplinary
Qandeel Saleem, Milad Torabfam, Tuce Fidan, Hasan Kurt, Meral Yuce, Nigel Clarke, Mustafa Kemal Bayazit
Summary: This article presents the use of microwave-promoted continuous flow systems in nanoparticle synthesis, discussing the impact of various parameters on nanoparticle properties and the advantages over batch processing. It also analyzes different microwave continuous flow reactors and nanosynthesis routes, emphasizes the importance of numerical modeling, and looks ahead to future prospects of this technology.
ACS SUSTAINABLE CHEMISTRY & ENGINEERING
(2021)
Article
Chemistry, Organic
Jian Qiu, Cece Wang, Lu Zhou, Yixian Lou, Kai Yang, Qiuling Song
Summary: In this study, an efficient protocol for the construction of gem-difluorohomoallylic boronates was developed through a nickel-catalyzed radical promoted defluoroalkylborylation reaction under mild conditions, using α-trifluoromethyl alkenes and α-haloboronates as substrates. This reaction demonstrated a broad substrate scope, good functional group tolerance, and diverse transformations.
Article
Chemistry, Multidisciplinary
Jorge Tovar-Rodriguez, Emiliano Fratini, Piero Baglioni, Carlo Ferrari, Jose Antonio de los Reyes-heredia, Yonatan Ramirez-Hernandez, Ignacio Rene Galindo-Esquivel
Summary: Solvothermal synthesis of mesoporous materials based on amphiphilic molecules as structure-directing agents can be enhanced using non-conventional technologies for stirring and thermal activation. Here, we disclose a green synthesis approach for the preparation of cerium-modified hexagonally ordered silica sieves. Ultrasound micromixing enabled us to obtain well-dispersed Ce in the self-assembled silica network and yielded ordered materials with high cerium content (Ce/Si molar ratio = 0.08). Microwave dielectric heating, applied by an innovative open-end coaxial antenna, was used to reduce the overall hydrothermal synthesis time and to improve the surface area and textural properties. These mesoporous materials were used as a Ni catalyst support (10 wt.% metal loading) for the ethanol steam reforming reaction. The new catalysts featured complete ethanol conversion, high H-2 selectivity (65%) and better stability, compared to the same catalyst prepared with magnetic stirring and conventional heating. The Ce-promoted silica sieves offered a suitable support for the controlled growth of nanocarbon that does not result in catalyst deactivation or poisoning after 6 h on stream.
Article
Neurosciences
Yanxiao Li, Yee Ling Ng, Manish D. Paranjpe, Qi Ge, Fengyun Gu, Panlong Li, Shaozhen Yan, Jie Lu, Xiuying Wang, Yun Zhou
Summary: This study aimed to improve the statistical power in detecting changes in brain glucose metabolism, amyloid, and tau deposition in Alzheimer's disease studies by using a reference tissue-based quantification approach. The results showed that the tracer-specific reference tissue improved the detection of PET SUVR changes, which is beneficial for early diagnosis, disease progression monitoring, and therapeutic response in Alzheimer's disease.
HUMAN BRAIN MAPPING
(2022)
Article
Biochemistry & Molecular Biology
Lindsey R. Drake, Allen F. Brooks, Anthony J. Mufarreh, Jonathan M. Pham, Robert A. Koeppe, Xia Shao, Peter J. H. Scott, Michael R. Kilbourn
ACS CHEMICAL NEUROSCIENCE
(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)
Article
Cardiac & Cardiovascular Systems
David M. Raffel, Yong-Woon Jung, Robert A. Koeppe, Keun Sam Jang, Guie Gu, Peter J. H. Scott, Venkatesh L. Murthy, Jill Rothley, Kirk A. Frey
CIRCULATION-CARDIOVASCULAR IMAGING
(2018)
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)
