Fluorine-18 labeling of peptides and proteins.

The pool of promising peptides worthy of investigation and evaluation for clinical use is continuously filled from different sources. Driven by the promising results obtained with peptides addressing somatostatin-2 receptor positive (sst2+) neuroendocrine tumours, other peptides targeting further receptor systems are being studied and evaluated. Progress in profiling the density and incidence of peptide hormone receptors in human cancer has initiated and will further promote research on the corresponding peptidic binders. In addition, industrial pharmaceutical research will be another significant source of peptides in the future. A recent prognosis revealed that about 50% of the drugs entering clinical trials in the next years will be peptides. The extensive research activities in genomics and proteomics will point out and quantify new and already known target structures upregulated in specific diseases. Based on the knowledge of their endogenous ligands or via selection of suitable candidates by phage display, suitable peptide ligands for e.g. membrane associated receptors can be identified and thus allow targeting of such binding sites. Thus, bioactive peptides specifically addressing relevant molecular targets are expected to become an important class of tracers, also due to the possibility of bridging imaging with therapeutic approaches. In this brief overview a summary of methods and strategies for the 18F-labeling of peptides and proteins is given.