TY - JOUR
T1 - Increased cell death after therapy with an Arg-Gly-Asp-linked somatostatin analog
AU - Capello, Astrid
AU - Krenning, Eric P.
AU - Bernard, Bert F.
AU - Breeman, Wout A.P.
AU - Van Hagen, Martin P.
AU - De Jong, Marion
PY - 2004/10/1
Y1 - 2004/10/1
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=16544369187&partnerID=8YFLogxK
UR - https://www.researchgate.net/publication/8243631_Increased_Cell_Death_After_Therapy_with_an_Arg-Gly-Asp-Linked_Somatostatin_Analog
M3 - Article
C2 - 15471839
AN - SCOPUS:16544369187
SN - 0161-5505
VL - 45
SP - 1716
EP - 1720
JO - Journal of Nuclear Medicine
JF - Journal of Nuclear Medicine
IS - 10
ER -