Design and preclinical evaluation of a novel apelin-based PET radiotracer targeting APJ receptor for molecular imaging of angiogenesis
| dc.rights.license | open | en_US |
| dc.contributor.author | LOUIS, Beatrice | |
| dc.contributor.author | NAIL, Vincent | |
| dc.contributor.author | NACHAR, Oriane | |
| dc.contributor.author | BOUHLEL, Ahlem | |
| dc.contributor.author | MOYON, Anais | |
| dc.contributor.author | BALASSE, Laure | |
| dc.contributor.author | SIMONCINI, Stephanie | |
| dc.contributor.author | CHABERT, Adrien | |
| dc.contributor.author | FERNANDEZ, Samantha | |
| dc.contributor.author | BRIGE, Pauline | |
| dc.contributor.author | HACHE, Guillaume | |
| dc.contributor.author | TINTARU, Aura | |
| hal.structure.identifier | Institut de Neurosciences cognitives et intégratives d'Aquitaine [INCIA] | |
| dc.contributor.author | MORGAT, Clement | |
| dc.contributor.author | DIGNAT-GEORGE, Francoise | |
| dc.contributor.author | GARRIGUE, Philippe | |
| dc.contributor.author | GUILLET, Benjamin | |
| dc.date.accessioned | 2023-06-28T08:01:36Z | |
| dc.date.available | 2023-06-28T08:01:36Z | |
| dc.date.issued | 2023-03-27 | |
| dc.identifier.issn | 1573-7209 | en_US |
| dc.identifier.uri | https://oskar-bordeaux.fr/handle/20.500.12278/182849 | |
| dc.description.abstractEn | APJ has been extensively described in the pathophysiology of angiogenesis and cell proliferation. The prognostic value of APJ overexpression in many diseases is now established. This study aimed to design a PET radiotracer that specifically binds to APJ. Apelin-F13A-NODAGA (AP747) was synthesized and radiolabeled with gallium-68 ([Ga]Ga-AP747). Radiolabeling purity was excellent (> 95%) and stable up to 2 h. Affinity constant of [Ga]Ga-AP747 was measured on APJ-overexpressing colon adenocarcinoma cells and was in nanomolar range. Specificity of [Ga]Ga-AP747 for APJ was evaluated in vitro by autoradiography and in vivo by small animal PET/CT in both colon adenocarcinoma mouse model and Matrigel plug mouse model. Dynamic of [Ga]Ga-AP747 PET/CT biodistributions was realized on healthy mice and pigs for two hours, and quantification of signal in organs showed a suitable pharmacokinetic profile for PET imaging, largely excreted by urinary route. Matrigel mice and hindlimb ischemic mice were submitted to a 21-day longitudinal follow-up with [Ga]Ga-AP747 and [Ga]Ga-RGD small animal PET/CT. [Ga]Ga-AP747 PET signal in Matrigel was significantly more intense than that of [Ga]Ga-RGD. Revascularization of the ischemic hind limb was followed by LASER Doppler. In the hindlimb, [Ga]Ga-AP747 PET signal was more than twice higher than that of [Ga]Ga-RGD on day 7, and significantly superior over the 21-day follow-up. A significant, positive correlation was found between the [Ga]Ga-AP747 PET signal on day 7 and late hindlimb perfusion on day 21. We developed a new PET radiotracer that specifically binds to APJ, [Ga]Ga-AP747 that showed more efficient imaging properties than the most clinically advanced tracer of angiogenesis, [Ga]Ga-RGD. | |
| dc.description.sponsorship | France Life Imaging | en_US |
| dc.language.iso | EN | en_US |
| dc.rights | Attribution 3.0 United States | * |
| dc.rights.uri | http://creativecommons.org/licenses/by/3.0/us/ | * |
| dc.subject.en | Angiogenesis | |
| dc.subject.en | Apelin | |
| dc.subject.en | APJ | |
| dc.subject.en | PET imaging | |
| dc.subject.en | Theranostics | |
| dc.title.en | Design and preclinical evaluation of a novel apelin-based PET radiotracer targeting APJ receptor for molecular imaging of angiogenesis | |
| dc.title.alternative | Angiogenesis | en_US |
| dc.type | Article de revue | en_US |
| dc.identifier.doi | 10.1007/s10456-023-09875-8 | en_US |
| dc.identifier.pubmed | 36973482 | en_US |
| bordeaux.journal | Angiogenesis | en_US |
| bordeaux.hal.laboratories | Institut de neurosciences cognitives et intégratives d'Aquitaine (INCIA) - UMR 5287 | en_US |
| bordeaux.institution | Université de Bordeaux | en_US |
| bordeaux.institution | CNRS | en_US |
| bordeaux.team | Imagerie multimodale translationnelle | |
| bordeaux.peerReviewed | oui | en_US |
| bordeaux.inpress | non | en_US |
| bordeaux.import.source | pubmed | |
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| hal.export | true | |
| workflow.import.source | pubmed | |
| dc.rights.cc | CC BY-NC-ND | en_US |
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