Radiometallation of receptor-specific peptides for diagnosis and treatment of human cancer.

Radiolabeled, receptor-specific peptides are becoming increasingly popular as targeting vectors for the design and development of new diagnostic and therapeutic radiopharmaceuticals. The over-expression of functioning receptors on a variety of human cancers makes this method of drug development a viable tool for tumor targeting in vivo. This review describes some of the more recent efforts that are currently underway towards development of new receptor-specific radiopharmaceuticals. Diagnostic/therapeutic radionuclides, specific metal co-ordinating ligands/chelating systems, spacer technology, radiolabeling protocols, and specific peptides/peptide conjugates will be discussed in detail.