[Protein- and peptide-derived radiopharmaceuticals].
Recent development of radiochemistry has provided various reagent that allow stable attachment of radiolabels to proteins in vivo. The advent of genetic and protein engineering have generated proteins and peptides with reduced or no immunogenicity or more favorable distribution characteristics. However, localization of radioactivity in nontarget tissues still constitutes a problem to be resolved for accurate diagnosis and effective therapy using the radiopharmaceuticals. Recent studies have indicated that radiometabolites after lysosomal proteolysis of proteins play a critical role in the radioactivity levels in nontarget tissues. Furthermore, radiochemical design of polypeptides that liberates radiometabolites of rapid urinary excretion after lysosomal proteolysis in nontarget tissues has facilitated rapid radioactivity elimination from nontarget tissues to urine. From these findings, we believe a new era of protein- and peptide-derived radiopharmaceuticals much more suitable for diagnostic and therapeutic applications will be opened soon.
Arano
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Y
Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University.
D000818:Animals; D006801:Humans; D004369:Pentetic Acid; D010455:Peptides / Q000737:chemistry; D011506:Proteins / Q000737:chemistry; D011854:Radiochemistry; D019275:Radiopharmaceuticals
D010455:Peptides; D011506:Proteins; D019275:Radiopharmaceuticals; D004369:Pentetic Acid