Candidates for Peptide Receptor Radiotherapy Today and in the Future
Jean Claude Reubi, MD1,
Helmut R. Mäcke, PhD2 and
Eric P. Krenning, MD3
1 Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Berne, Switzerland
2 Radiopharmacy, Department of Nuclear Medicine, University Hospital Basel, Basel, Switzerland
3 Department of Nuclear Medicine, Erasmus Medical Center, Rotterdam, The Netherlands
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FIGURE 1. Homogeneous distribution of somatostatin receptors in a GEP NET (A–C) and nonhomogeneous distribution in a breast cancer (D–F). (A and D) Hematoxylin-eosin stained sections. Bars = 1 mm. (B and E) Total binding of 125I-Tyr3-octreotide with homogenous distribution in B but not in E. (C and F) Nonspecific binding.
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FIGURE 2. Concomitant but complementary distribution of CCK and somatostatin receptors in adjacent sections of GEP NET. (A) Hematoxylin-eosin stained section. Bar = 1 mm. (B) Autoradiograph showing CCK receptors predominantly expressed in right part of tumor. (C) Autoradiograph showing somatostatin receptors predominantly found in left part of tumor.
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FIGURE 3. Chemical structures of DTPA- and DOTA-modified somatostatin-based peptides for targeted radiotherapy. (A) DTPA0-octreotide. (B) DOTA0-Tyr3-octreotide (DOTATOC). (C) DOTA0-Tyr3-Thr8-octreotide (DOTATATE). (D) DOTA0-2-Nal-Tyr3-Thr-NH28-octreotide (DOTA-lanreotide).
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FIGURE 4. Structural formula of the CCK2-selective analog DTPA-D-Glu-Glu5-Ala-Tyr-Gly-Trp-Met-Asp-PheNH2 (minigastrin).
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FIGURE 5. Structural formula of 90Y-DOTAGA-substance P.
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FIGURE 6. Structural formula of KE 108 (pan-somatostatin).
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Copyright © 2005 by the Society of Nuclear Medicine.
