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.
Giblin
Michael F
MF
The Hany S Truman Memorial Veterans' Hospital, Columbia, MO 65201, USA.
Veerendra
Bhadrasetty
B
Smith
Charles J
CJ
D000818:Animals; D006801:Humans; D007553:Isotope Labeling / Q000379:methods; D008024:Ligands; D009369:Neoplasms / Q000175:diagnosis* / Q000188:drug therapy*; D036361:Peptide Hormones / Q000493:pharmacokinetics*; D010455:Peptides / Q000378:metabolism / Q000627:therapeutic use; D011868:Radioisotopes / Q000737:chemistry / Q000493:pharmacokinetics*; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics / Q000627:therapeutic use; D018000:Receptors, Peptide / Q000378:metabolism*
D008024:Ligands; D036361:Peptide Hormones; D010455:Peptides; D011868:Radioisotopes; D019275:Radiopharmaceuticals; D018000:Receptors, Peptide