One-step 18F-labeling of peptides for positron emission tomography imaging using the SiFA methodology

• Verfasst von: Wängler, Carmen [VerfasserIn]
• Verfasst von: Niedermoser, Sabrina [VerfasserIn]
• Verfasst von: Wängler, Björn [VerfasserIn]
• Titel: One-step 18F-labeling of peptides for positron emission tomography imaging using the SiFA methodology
• Verf.angabe: Carmen Wängler, Sabrina Niedermoser, Joshua Chin, Katy Orchowski, Esther Schirrmacher, Klaus Jurkschat, Liuba Iovkova-Berends, Alexey P. Kostikov, Ralf Schirrmacher, Björn Wängler
• E-Jahr: 2012
• Jahr: 04 October 2012
• Umfang: 10 S.
• Fussnoten: Im Titel ist 18 hochgestellt ; Korrigierte Version: 23.10.2012, Korrektur betrifft Schreibweise der Autorin Katy Orchowski ; Gesehen am 09.07.2018
• Titel Quelle: Enthalten in: Nature protocols
• Ort Quelle: Basingstoke : Nature Publishing Group, 2006
• Jahr Quelle: 2012
• Band/Heft Quelle: 7(2012), 11, Seite 1946-1955
• ISSN Quelle: 1750-2799
• DOI: doi:10.1038/nprot.2012.109
• Datenträger: Online-Ressource
• Sprache: eng
• K10plus-PPN: 1577394909

Abstract

Here we present a procedure to label peptides with the positron-emitting radioisotope fluorine-18 (18F) using the silicon-fluoride acceptor (SiFA) labeling methodology. Positron emission tomography (PET) has gained high importance in noninvasive imaging of various diseases over the past decades, and thus new specific imaging probes for PET imaging, especially those labeled with 18F, because of the advantageous properties of this nuclide, are highly sought after. N-terminally SiFA-modified peptides can be labeled with 18F− in one step at room temperature (20-25 °C) or below without forming side products, thereby producing satisfactory radiochemical yields of 46 ± 1.5% (n = 10). The degree of chemoselectivity of the 18F-introduction, which is based on simple isotopic exchange, allows for a facile cartridge-based purification fully devoid of HPLC implementation, thereby yielding peptides with specific activities between 44.4 and 62.9 GBq μmol−1 (1,200-1,700 Ci mmol−1) within 25 min.