Abstract
Radiolabelled peptides have shown to be an important class of radiopharmaceuticals for imaging and therapy of malignancies expressing receptors of regulatory peptides. These peptides have high affinity and specificity for their receptors. The majority of these receptors are present at different levels in different tissues and tumours. This review focuses on the application of regulatory peptides radiolabelled with 67/68Ga , 90Y, 111In or 177Lu. Due attention is given to the current status of research, limitations and future perspectives of the application of these radiolabelled peptides for imaging and radiotherapy. It also covers elements of the basic science and preclinical and clinical aspects in general, however, mostly based on somatostatin receptor-mediated imaging and therapy. New analogues, chelators, radionuclides and combinations thereof are discussed.
Keywords: somatostatin, scintigraphy, peptide receptor-targeted radiotherapy, radiolabelling, DTPA, DOTA, receptor, gastrin-releasing peptide, bombesin, substance P
Anti-Cancer Agents in Medicinal Chemistry
Title: Radiolabelled Regulatory Peptides for Imaging and Therapy
Volume: 7 Issue: 3
Author(s): M. de Jong, T. J. Visser, E. de Blois, W. A. P. Breeman, D. J. Kwekkeboom and E. P. Krenning
Affiliation:
Keywords: somatostatin, scintigraphy, peptide receptor-targeted radiotherapy, radiolabelling, DTPA, DOTA, receptor, gastrin-releasing peptide, bombesin, substance P
Abstract: Radiolabelled peptides have shown to be an important class of radiopharmaceuticals for imaging and therapy of malignancies expressing receptors of regulatory peptides. These peptides have high affinity and specificity for their receptors. The majority of these receptors are present at different levels in different tissues and tumours. This review focuses on the application of regulatory peptides radiolabelled with 67/68Ga , 90Y, 111In or 177Lu. Due attention is given to the current status of research, limitations and future perspectives of the application of these radiolabelled peptides for imaging and radiotherapy. It also covers elements of the basic science and preclinical and clinical aspects in general, however, mostly based on somatostatin receptor-mediated imaging and therapy. New analogues, chelators, radionuclides and combinations thereof are discussed.
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Cite this article as:
de Jong M., Visser J. T., de Blois E., P. Breeman A. W., Kwekkeboom J. D. and Krenning P. E., Radiolabelled Regulatory Peptides for Imaging and Therapy, Anti-Cancer Agents in Medicinal Chemistry 2007; 7 (3) . https://dx.doi.org/10.2174/187152007780618171
DOI https://dx.doi.org/10.2174/187152007780618171 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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