Two-step methodology for high-yield routine radiohalogenation of peptides: (18)F-labeled RGD and octreotide analogs.

Abstract

Oxime formation between aminooxy-functionalized peptides and an (18)F-labeled aldehyde or ketone-in this case, [(18)F]FB-CHO-combines fast 1-step, high-yield synthesis of an (18)F-labeled prosthetic group stable against in vivo defluorination with rapid, 1-step chemoselective conjugation to unprotected peptides under mild conditions. Thus, it allows fast and straightforward large-scale production of (18)F-labeled peptides for clinical routine PET application. Furthermore, it opens new perspectives to peptide radiohalogenation in general, permitting labeling of the same precursor both with diagnostic ((18)F, (124)I, (120 g)I, (123)I) and therapeutic ((211)At, (131)I) radiohalogens.