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

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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Bioorganic & medicinal chemistry, Elsevier, 2010, 18 (14), pp.5400-12. 〈10.1016/j.bmc.2010.05.031〉
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Contributeur : Marc Poirot <>
Soumis le : samedi 18 septembre 2010 - 15:30:36
Dernière modification le : jeudi 11 janvier 2018 - 06:15:23

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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 & medicinal chemistry, Elsevier, 2010, 18 (14), pp.5400-12. 〈10.1016/j.bmc.2010.05.031〉. 〈inserm-00519158〉

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