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ACS Chem Biol. 2016 Jun 17;11(6):1587-94. doi: 10.1021/acschembio.6b00172. Epub 2016 Mar 31.

Site-Specific Radiofluorination of Biomolecules with 8-[(18)F]-Fluorooctanoic Acid Catalyzed by Lipoic Acid Ligase.

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Department of Radiology and Biomedical Imaging, University of California San Francisco , Suite 350, 185 Berry Street, San Francisco, California 94107, United States.
Department of Pharmaceutical Chemistry, University of California San Francisco , Genentech Hall, S-514, 600 16th Street, San Francisco, California 94158, United States.


New methodologies for site-specifically radiolabeling proteins with (18)F are required to generate high quality radiotracers for preclinical and clinical applications with positron emission tomography. Herein, we report an approach by which we use lipoic acid ligase (LplA) to conjugate [(18)F]-fluorooctanoic acid to an antibody fragment bearing the peptide substrate of LplA. The mild conditions of the reaction preserve antibody immunoreactivity, and the efficiency of LplA allows for >90% yield even with very small amounts of peptidic precursor (1-10 nmol). These features are advantageous compared to the current gold standard in the field. Moreover, the methodology introduces a new application for an important tool in chemical biology.

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