Al18F labeling of peptides and proteins

Radiolabeled receptor-binding peptides and proteins have emerged as an important class of radiopharmaceuticals that have changed radionuclide imaging in clinical practice. Many strategies have been developed to radiolabel these peptide and proteins with fluorine-18. The majority of these methods is time-consuming and suffer from low yields. A more straightforward approach was proposed a few years ago, based on the chelation of aluminum fluoride by (1,4,7-triazacyclononane-1,4,7-triacetic acid). This approach has been optimized with regard to labeling yield and specific activity. In addition, crystallography studies have led to the design of optimized chelators. Subsequently, the (AlF)-F-18 technology is finding widespread use in labeling peptides and proteins. Various hapten peptides for pre-targeting studies have been labeled with (AlF)-F-18, as well as (v3) integrin-binding peptides have been studied, and also larger peptides, such as exendin-4 and affibody molecules and heat-labile proteins have been labeled with (AlF)-F-18. Here, we summarize the development, optimization, and applications of the (AlF)-F-18 labeling technology. (c) 2013 The Authors. J. Label Compd. Radiopharm published by John Wiley & Sons Ltd.