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Development of a new radioligand for cholecystokinin receptor subtype 2 scintigraphy: from molecular modeling to in vivo evaluation.

Séverine Brillouet 1, 2 Sandra Dorbes 1 Frédéric Courbon 1, 2, 3 Claude Picard 4 Jean Pierre Delord 5 Eric Benoist 4 Marc Poirot 1 Béatrice Mestre-Voegtlé 4 Sandrine Silvente-Poirot 1
1 Departement /u563 : Oncogenèse, Signalisation et Innovation thérapeutique
CPTP - Centre de Physiopathologie Toulouse Purpan, Institut Claudius Regaud
2 Département d'Imagerie Médicale [Toulouse]
3 Service d'anatomie pathologique et histologie-cytologie [Rangueil]
4 SPCMIB - Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique
5 Laboratoire de Pharmacologie Clinique et Expérimentale des Médicaments Anticancéreux
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.
keyword : Metal chelate Gastrin receptor 111Indium Metal conjugate SPECT Cancer
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https://www.hal.inserm.fr/inserm-00519158
Contributor : Marc Poirot <>
Submitted on : Saturday, September 18, 2010 - 3:30:36 PM
Last modification on : Friday, March 12, 2021 - 1:32:08 PM

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INSERM | CNRS | INC-CNRS | UNIV-TLSE3 | INFINITY

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Séverine Brillouet, Sandra Dorbes, Frédéric Courbon, Claude Picard, Jean Pierre Delord, et al.. Development of a new radioligand for cholecystokinin receptor subtype 2 scintigraphy: from molecular modeling to in vivo evaluation.. Bioorganic and Medicinal Chemistry, Elsevier, 2010, 18 (14), pp.5400-12. ⟨10.1016/j.bmc.2010.05.031⟩. ⟨inserm-00519158⟩

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