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Oncotarget. 2018 May 15;9(37):24693-24706. doi: 10.18632/oncotarget.25266. eCollection 2018 May 15.

Potentiation of 177Lu-octreotate peptide receptor radionuclide therapy of human neuroendocrine tumor cells by PARP inhibitor.

Purohit NK1,2,3, Shah RG1,2,3, Adant S1,2,3,4,5, Hoepfner M6, Shah GM1,2,3, Beauregard JM2,4,5.

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Department of Molecular Biology, Medical Biochemistry and Pathology, Université Laval, Quebec City, Canada.
Cancer Research Center, Université Laval, Quebec City, Canada.
Neurosciences and Oncology Branches of CHU de Québec, Université Laval Research Center, Quebec City, Canada.
Department of Radiology and Nuclear Medicine, Université Laval, Quebec City, Canada.
Oncology Branch of CHU de Québec, Université Laval Research Center, Quebec City, Canada.
Institute of Physiology, Charité-Universitätsmedizin Berlin, Berlin, Germany.


For patients with inoperable neuroendocrine tumors (NETs) expressing somatostatin receptors, peptide receptor radionuclide therapy (PRRT) with 177Lu-[DOTA0-Tyr3]-octreotate (177Lu-octreotate) is one of the most promising targeted therapeutic options but it rarely achieves cure. Therefore, different approaches are being tested to increase the efficacy of 177Lu-octreotate PRRT in NET patients. Using the gastroenteropancreatic BON-1 and the bronchopulmonary NCI-H727 as NET cell models, here we report that pharmacological inhibitors of DNA repair-associated enzyme poly(ADP-ribose) polymerase-1 (PARPi) potentiate the cytotoxic effect of 177Lu-octreotate on 2D monolayer and 3D spheroid models of these two types of NET cells. PARPi mediates this effect by enhancing 177Lu-octreotate-induced cell cycle arrest and cell death. Thus, the use of PARPi may offer a novel option for improving the therapeutic efficacy of 177Lu-octreotate PRRT of NETs.


177Lu-octreotate; PARP inhibitor; neuroendocrine tumors; peptide receptor radionuclide therapy; radiosensitization

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