Development of a new radioligand for cholecystokinin receptor subtype 2 scintigraphy: from molecular modeling to in vivo evaluation. - Archive ouverte HAL Access content directly
Journal Articles Bioorganic and Medicinal Chemistry Year : 2010

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

(1, 2) , (1) , (1, 2, 3) , (4) , (5) , (4) , (1) , (4) , (1)
1
2
3
4
5

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.
Not file

Dates and versions

inserm-00519158 , version 1 (18-09-2010)

Identifiers

Cite

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, 2010, 18 (14), pp.5400-12. ⟨10.1016/j.bmc.2010.05.031⟩. ⟨inserm-00519158⟩
151 View
0 Download

Altmetric

Share

Gmail Facebook Twitter LinkedIn More