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Journal articles
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.
https://www.hal.inserm.fr/inserm-00519158
Contributor : Marc Poirot <>
Submitted on : Saturday, September 18, 2010 - 3:30:36 PM
Last modification on : Thursday, February 18, 2021 - 3:32:01 PM
Contributor : Marc Poirot <>
Submitted on : Saturday, September 18, 2010 - 3:30:36 PM
Last modification on : Thursday, February 18, 2021 - 3:32:01 PM