From Carbon-11-Labeled Amino Acids to Peptides in Positron Emission Tomography: the Synthesis and Clinical Application Aleksandra Pekošak, Ulrike Filp, Alex J
Mol Imaging Biol (2018) DOI: 10.1007/s11307-018-1163-5 * The Author(s), 2018. This article is an open access publication REVIEW ARTICLE From Carbon-11-Labeled Amino Acids to Peptides in Positron Emission Tomography: the Synthesis and Clinical Application Aleksandra Pekošak, Ulrike Filp, Alex J. Poot, Albert D. Windhorst Radionuclide Center, Department of Radiology and Nuclear Medicine, VU University Medical Center, De Boelelaan 1085c, 1081 HV, Amsterdam, The Netherlands Abstract Radiolabeled amino acids, their derivatives and peptides have a broad scope of application and can be used as receptor ligands, as well as enzyme substrates for many different diseases as radiopharmaceutical tracers. Over the past few decades, the application of molecular imaging techniques such as positron emission tomography (PET) has gained considerable importance and significance in diagnosis in today’s advanced health care. Next to that, the availability of cyclotrons and state-of-the-art radiochemistry facilities has progressed the production of imaging agents enabling the preparation of many versatile PET radiotracers. Due to many favorable characteristics of radiolabeled amino acids and peptides, they can be used for tumor staging and monitoring the progress of therapy success, while aromatic amino acids can be employed as PET tracer to study neurological disorders. This review provides a comprehensive overview of radiosynthetic and enzymatic approaches towards carbon-11 amino acids, their analogues and peptides, with focus on stereoselective reactions, and reflects upon their clinical application. Key Words: Carbon-11, Amino acid, Peptide, Radiolabeling, PET imaging Introduction D-glucose ([18F]FDG) as well as a large variety of other PET tracers like receptor ligands or enzyme substrates.
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