Development of a new radioligand for cholecystokinin receptor subtype 2 scintigraphy: From molecular modeling to in vivo evaluation |
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| Authors: | Séverine Brillouet Sandra Dorbes Frédéric Courbon Claude Picard Jean Pierre Delord Eric Benoist Marc Poirot Béatrice Mestre-Voegtlé Sandrine Silvente-Poirot |
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| Institution: | 1. INSERM 563, Equipe Marc Poirot «Métabolisme, Oncogenèse et Différenciation cellulaire», CPTP, Toulouse, France;2. Université Paul Sabatier Toulouse III, Toulouse, France;3. CNRS;Laboratoire de Synthèse et Physico-Chimie de Molécules d’Intérêt Biologique, SPCMIB, UMR-5068, Toulouse, France;4. Université Paul Sabatier Toulouse III, Laboratoire de Synthèse et Physico-Chimie de Molécules d’Intérêt Biologique, SPCMIB, Toulouse, France;5. Département d’Imagerie Médicale, Institut Claudius Regaud, Toulouse, France;6. CHU Rangueil, Toulouse, France;7. Institut Claudius Regaud et EA3035 Laboratoire de Pharmacologie Clinique et Expérimentale des Médicaments Anticancéreux, Toulouse, France |
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| Abstract: | To improve the targeting to tumors expressing the cholecystokinin receptor subtype 2 (CCK2R) with limited kidney uptake, we synthesized a novel cholecystokinin C-terminal tetrapeptide (CCK4)-based derivative conjugated to an original bipyridine-chelator (BPCA), 111In-BPCA-(Ahx)2-CCK4. To our knowledge this is the first CCK4-based radioligand that presents a high affinity for the CCK2R, a high and specific tumor uptake, a low renal accumulation and a very good visualization of tumors in vivo compared with an internal control, 111Indium-trans-cyclohexyldiethylenetriaminepenta-acetic acid-cholecystokinin octapeptide (111In-CHX-A″-DTPA-CCK8). These properties make 111In-BPCA-(Ahx)2-CCK4, a promising candidate for imaging and peptide receptor radionuclide therapy of CCK2R positive tumors. |
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