Increased cell death after therapy with an Arg-Gly-Asp-linked somatostatin analog

Astrid Capello*, Eric P. Krenning, Bert F. Bernard, Wout A.P. Breeman, Martin P. Van Hagen, Marion De Jong

*Corresponding author for this work

Research output: Contribution to journalArticleAcademicpeer-review

41 Citations (Scopus)
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Abstract

Receptor-targeted scintigraphy and radionuclide therapy with radiolabeled somatostatin analogs are successfully applied for somatostatin receptor-positive tumors. The synergistic effects of an apoptosis-inducing factor, for example, the Arg-Gly-Asp (RGD) motif, can increase the radiotherapeutic efficacy of these peptides. Hence, the tumoricidal effects of the hybrid peptide RGD-diethylaminetriaminepentaacetic acid (DTPA)-Tyr3-octreotate, hereafter referred to as RGD-DTPA-octreotate, were evaluated in comparison with those of RGD and Tyr 3-octreotate. Methods: The therapeutic effects of RGD-111In-DTPA-octreotate, 111In-DTPA-RGD, and 111In-DTPA-Tyr3-octreotate were investigated with various cell lines by use of a colony-forming assay, and caspase-3 activity was also determined. Results: Tumoricidal effects were found with 111In-DTPA-RGD, 111In-DTPA-Tyr3- octreotate, and RGD-111In-DTPA-octreotate, in order from least effective to most effective. Also, the largest increase in caspase-3 levels was found with RGD-111In-DTPA-octreotate. Conclusion: RGD- 111In-DTPA-octreotate has more pronounced tumoricidal effects than 111In-DTPA-RGD and 111In-DTPA-Tyr3-octreotate, because of increased apoptosis, as indicated by increased caspase-3 activity.

Original languageEnglish
Pages (from-to)1716-1720
Number of pages5
JournalJournal of Nuclear Medicine
Volume45
Issue number10
Publication statusPublished - 1 Oct 2004

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