The radiolabeling of proteins by the [18F]AlF method

A new ([F-18]AlF)(2+)-binding ligand that contains 1,4,7-triazacyclononane-1,4-diacetate (NODA) attached to a methyl phenylacetic acid group (MPA) was conjugated to N-(2-aminoethyl)maleimide (EM) to form NODA-MPAEM. The NODA-MPAEM was labeled with ([F-18]AlF)(2+) at 105 degrees C in 49-82% yield and conjugated at room temperature to an antibody Fab fragment in 69-80% yield (total time similar to 50 min) and with retention of immunoreactivity. These data indicate that the rapid and simple [F-18]AlF-labeling method can be easily adapted for preparing heat-sensitive compounds with F-18 quickly and in high yields. (C) 2011 Elsevier Ltd. All rights reserved.