The Challenge of Labeling Macromolecules with Fluorine-18: Three Decades of Research

Macromolecule-based radiopharmaceuticals are gaining in importance. Peptides selected by phage display, bioactive endogenous proteins, antibodies and their engineered derivatives, SELEX-evolved oligonucleotides as well as more recently nano-objects are sources of new potential targets for a radiolabeling for molecular imaging applications. This review aims at addressing in as much detail as possible the strategies that have been developed to radiofluorinate these entities which interest for imaging and medical applications does not need to be demonstrated anymore.