Authors: Jonathan Cotton, Simon Freisinger, Kerstin Fuchs, Christoph Goering, Andreas Maurer, Nicolas Beziere, Bernd J. PichlerWerner Siemens Imaging Center, Department of Preclinical Imaging and Radiopharmacy, Eberhard Karls University of Tuebingen, GermanyBackground α-Fucosidase (AF) is implicated in many pathologies e.g. cancer, senescence and inflammatory processes such as arthritis. The pyrrolidine 4-epi-(+)-Codonopsinine 1 is an AF inhibitor (AFi) with respective IC50 and Ki values of 58 nM of 10 nM.
Authors: Maia Zeni(1), Ma. Daniela Santi(1), Florencia Arredondo(1), Rosina Dapueto (1), Mariana Peralta(2,3), José Luis Cabrera(3), Ma. Gabriela Ortega(2,3), Ana Rey(4), Javier Giglio(1)1 – Centro Uruguayo de Imagenología Molecular (CUDIM), Montevideo, Uruguay2 - Laboratorio de Farmacognosia, Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Argentina3- Instituto Multidisciplinario de Biología Vegetal (IMBIV – CONICET), Argentina 3 – Área de Radioquímica, Facultad de Química, Universidad de la República, Uruguay
Position: CNRS Research associate, Center for Research in Cancerology and Immunology, Nantes, FranceEducation: PhD in organic chemistry, university of Nantes, FrancePost-doctoral fellow in radioimmune and inorganic chemistry at the National Cancer Institute (NIH), Bethesda MD, USAResearch: Radiolabeling chemistry with radiometals and radiohalogens, particularly astatine-211.
Authors: Carlos Alberto Rossatto Jr1, Rosemeire Aparecida Silva2, Ademar Benevolo Lugão3, Roger Chammas1, Carlos Alberto Buchpiguel1, Fabio Luiz Navarro Marques1. 1-Faculdade de Medicina da Universidade de Sao Paulo, Brazil 2-Instituto do Cancer do Estado de Sao Paulo, Hospital das Clinicas da Faculdade de Medicina da Universidade de Sao Paulo, Brazil 3- Instituto de Pesquisas Energeticas e Nucleares, Brazil
Authors: Flaviu Bulat1, 2, 3, Friederike Hesse1, Susana Ros1, Bala Atilli1, De-en Hu1, Connor J. Willmington-Holmes2, Dmitry Soloviev1, Franklin I. Aigbirhio3, Finian J. Leeper2, Kevin M. Brindle1, André A. Neves1 1 University of Cambridge, Cancer Research UK Cambridge Institute, Cambridge, United Kingdom 2 University of Cambridge, Department of Chemistry, Cambridge, United Kingdom 3 University of Cambridge, Wolfson Brain Imaging Centre, Cambridge, United Kingdom Background Cell death is an important target for imaging the early response of tumours to treatment. We have described recently 99mTc- and 111In-labelled derivatives of a phosphatidylserine-binding protein (C2Am) for imaging tumour cell death in vivo using SPECT . Aims We describe here the development and in vivo testing of a 18F-labelled derivative of C2Am for PET imaging of tumour cell death following therapy. Methods A one-pot, two-step automated synthesis of N-(5-[18F]fluoropentyl)maleimide (60 min, 12% RCY) has been developed. This was used to label the single cysteine present in C2Am within 30 min (Am=212±30 GBq/µmol (n=3)). Binding of [18F]FPenM-C2Am was assessed pre- and post-treatment in vivo by dynamic PET imaging and biodistribution studies.
Authors: Bo Zhang1, Pierre Cheung1, Emmi Puuvuori1, Amin Mohammad1, Sofie Ye1, Olle Korsgren2, Luke Odell1, Olof Eriksson1, Jonas Eriksson1 1 Science for Life Laboratory, Department of Medicinal Chemistry, Uppsala University, Uppsala, Sweden; 2 Department of Immunology, Genetics and Pathology, Clinical Immunology, Uppsala University, Uppsala, Sweden
Authors: Marion Berdal1, Laurent Navarro1, Sébastien Gouard1, Séverine Marionneau-Lambot1, Mikaël Croyal2, Cyrille Alliot1,3, Joëlle Gaschet1, Michel Chérel1, Alain Faivre Chauvet1, Jean-François Gestin1, François Guérard1 1 Université de Nantes, CNRS, Inserm, CRCINA, F-44000 Nantes, France2 Plateau de Spectrométrie de Masse du CRNH, UMR 1280, Nantes, France 3 Arronax GIP, Saint-Herblain, France
Authors: Braeden A. Mair1,3, Moustafa H. Fouad2,3, Uzair S. Ismailani2,3, Maxime Munch2,3, Benjamin H. Rotstein1,2,3 1Department of Chemistry and Biomolecular Sciences, University of Ottawa, Ottawa, ON, Canada K1N 6N5; 2Department of Biochemistry, Microbiology and Immunology, University of Ottawa, Ottawa, ON, Canada K1H 8M5; 3University of Ottawa Heart Institute, Ottawa, ON, Canada K1Y 4W7
Authors: Yu-Peng Zhou1, Mohammad B. Haskali2, Karla M. Ramos-Torres1, Bo Yeun Yang2, Victor W. Pike2, Pedro Brugarolas1 1 Gordon Center for Medical Imaging, Department of Radiology, Massachusetts General Hospital and Harvard Medical School, Boston, MA, USA 2 Section of PET Radiopharmaceutical Sciences, National Institute of Mental Health, National Institutes of Health, Bethesda, MD, USA
Authors: Coralie M. Bonnemaire1, Albert D. Windhorst1, Jurriën W. Collet2, Eelco Ruijter2, Romano V. A. Orru2, Danielle J. Vugts1 1 Amsterdam UMC, Vrije Universiteit Amsterdam, Radiology & Nuclear Medicine(s), Amsterdam Institute of Molecular and Life Sciences (AIMMS), de Boelelaan 1117, Amsterdam, Netherlands 2 Department of Chemistry and Pharmaceutical Sciences, Amsterdam Institute of Molecular and Life Sciences (AIMMS), Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ Amsterdam, The Netherlands Background The radiochemists’ synthetic possibilities are limited, due to a lack of variation in building blocks for PET tracer synthesis. N-formamides are important building blocks for the synthesis of a large variety of biological active compounds1. As such they are also interesting for PET tracer synthesis upon labelling with carbon-11. Aims The aim was to develop a fast and easy synthesis method for 11C-labelled N-formamides and apply this in the synthesis of the long-acting β2 agonist: N-[formyl-11C]formoterol2. Methods 11C-labelled N-formamides were prepared in one-pot starting by reduction of cyclotron produced [11C]CO2 to [11C]formic acid3, followed by N-11C-formylation of an amine. The N-11C-formylation reaction was achieved using the coupling agent BOP in pyridine. The synthesis route was developed using benzylamine as model substrate and was extended to other amines. Results and Conclusion N-[formyl-11C]benzylformamide could be isolated in 40±9% radiochemical yield, with 87±10% radiochemical purity and a molar activity higher than 100GBq/µmol in less than 26 min from EOB (n=3). A small series of 11C-labelled N-formamides was obtained with similar yields. This method will now be applied in the synthesis of N-[formyl-11C]formoterol.