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Your search keyword '"Prignon, A."' showing total 5 results
Start Over Author "Prignon, A." Journal journal of medicinal chemistry
5 results on '"Prignon, A."'

1. Positron Emission Tomography Imaging of Neurotensin Receptor-Positive Tumors with

Author

Emma, Renard, Mathieu, Moreau, Pierre-Simon, Bellaye, Mélanie, Guillemin, Bertrand, Collin, Aurélie, Prignon, Franck, Denat, and Victor, Goncalves

Subjects
Mice, Cell Line, Tumor, Neoplasms, Positron-Emission Tomography, Imidazoles, Animals, Humans, Receptors, Neurotensin, Adamantane, Gallium Radioisotopes, Radiopharmaceuticals, Chelating Agents
Abstract

Neurotensin receptor 1 (NTS

Published
2021

4. Design of Bimodal Ligands of Neurotensin Receptor 1 for Positron Emission Tomography Imaging and Fluorescence-Guided Surgery of Pancreatic Cancer

Author

Renard, Emma, Dancer, Pierre-Alix, Portal, Christophe, Denat, Franck, Prignon, Aurélie, and Goncalves, Victor

Abstract

Neurotensin receptor 1 (NTSR1) is overexpressed in most human pancreatic ductal adenocarcinomas. It makes it an attractive target for the development of pancreatic cancer imaging agents. In this study, we sought to develop a bimodal positron emission tomography (PET)/fluorescent imaging agent capable of specifically targeting these receptors. Starting from the structure of a known NTSR1 agonist, a series of tracers were synthesized, radiometalated with gallium-68, and evaluated in vitroand in vivo, in mice bearing an AsPC-1 xenograft. PET imaging allowed us to identify the compound [68Ga]Ga-NODAGA-Lys(Cy5**)-AEEAc-[Me-Arg8,Tle12]-NT(7–13) as the one with the most promising biodistribution profile, characterized by high tumor uptake (2.56 ± 0.97%ID/g, 1 h post-injection) and rapid elimination from nontargeted organs, through urinary excretion. Fluorescence imaging gave similar results. On this basis, fluorescence-guided resection of tumor masses was successfully carried out on a preclinical model.

Published
2020
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5. Positron Emission Tomography Imaging of Neurotensin Receptor-Positive Tumors with 68 Ga-Labeled Antagonists: The Chelate Makes the Difference Again.

Author

Renard E, Moreau M, Bellaye PS, Guillemin M, Collin B, Prignon A, Denat F, and Goncalves V

Subjects
Adamantane chemical synthesis, Adamantane chemistry, Adamantane pharmacokinetics, Animals, Cell Line, Tumor, Chelating Agents chemical synthesis, Chelating Agents pharmacokinetics, Gallium Radioisotopes chemistry, Humans, Imidazoles chemical synthesis, Imidazoles pharmacokinetics, Mice, Neoplasms metabolism, Positron-Emission Tomography, Radiopharmaceuticals chemical synthesis, Radiopharmaceuticals pharmacokinetics, Adamantane analogs & derivatives, Chelating Agents chemistry, Imidazoles chemistry, Neoplasms diagnostic imaging, Radiopharmaceuticals chemistry, Receptors, Neurotensin metabolism
Abstract

Neurotensin receptor 1 (NTS 1 ) is involved in the development and progression of numerous cancers, which makes it an interesting target for the development of diagnostic and therapeutic agents. A small molecule NTS 1 antagonist, named [ 177 Lu]Lu-IPN01087, is currently evaluated in phase I/II clinical trials for the targeted therapy of neurotensin receptor-positive cancers. In this study, we synthesized seven compounds based on the structure of NTS 1 antagonists, bearing different chelating agents, and radiolabeled them with gallium-68 for PET imaging. These compounds were evaluated in vitro and in vivo in mice bearing a HT-29 xenograft. The compound [ 68 Ga]Ga-bisNODAGA- 16 showed a promising biodistribution profile with mainly signal in tumor (4.917 ± 0.776%ID/g, 2 h post-injection). Its rapid clearance from healthy tissues led to high tumor-to-organ ratios, resulting in highly contrasted PET images. These results were confirmed on subcutaneous xenografts of AsPC-1 tumor cells, a model of NTS 1 -positive human pancreatic adenocarcinoma.

Published
2021
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