Anti-Cancer Agents in Medicinal Chemistry

(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Michelle Prudhomme  
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France

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Radiolabelled Regulatory Peptides for Imaging and Therapy

Author(s): M. de Jong, T. J. Visser, E. de Blois, W. A. P. Breeman, D. J. Kwekkeboom, E. P. Krenning.

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

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Article Details

VOLUME: 7
ISSUE: 3
Page: [345 - 357]
Pages: 13
DOI: 10.2174/187152007780618171
Price: $58