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Synthesis of Peptide Radiopharmaceuticals for the Therapy and Diagnosis of Tumor Diseases

Department of Nuclear Medicine, University Hospital Heidelberg, Im Neuenheimer Feld 400, D-69120 Heidelberg, Germany
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Molecules 2013, 18(3), 3379-3409; https://doi.org/10.3390/molecules18033379
Received: 29 December 2012 / Revised: 25 February 2013 / Accepted: 7 March 2013 / Published: 14 March 2013
(This article belongs to the Special Issue Chemical Protein and Peptide Synthesis)
Despite the advances in molecular biology and biochemistry, the prognosis of patients suffering from tumor diseases remains poor. The limited therapeutic success can be explained by the insufficient performance of the common chemotherapeutic drugs that lack the ability to specifically target tumor tissues. Recently peptide radiopharmaceuticals have been developed that enable the concurrent imaging and therapy of tumors expressing a specific target. Here, with a special emphasis on the synthesis of the building blocks required for the complexation of metallic radioisotopes, the requirements to the design and synthesis of radiolabeled peptides for clinical applications are described. View Full-Text
Keywords: radionuclides; chelator; prosthetic groups; carrier molecules; peptides; medicinal application; radiopharmaceutical; diagnostic imaging; radiotherapeutics radionuclides; chelator; prosthetic groups; carrier molecules; peptides; medicinal application; radiopharmaceutical; diagnostic imaging; radiotherapeutics
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Jamous, M.; Haberkorn, U.; Mier, W. Synthesis of Peptide Radiopharmaceuticals for the Therapy and Diagnosis of Tumor Diseases. Molecules 2013, 18, 3379-3409.

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