In VitroandIn VivoEvaluation of64Cu-Radiolabeled KCCYSL Peptides for Targeting Epidermal Growth Factor Receptor-2 in Breast Carcinomas
作者： Senthil R. Kumar , Fabio A. Gallazzi , Riccardo Ferdani , Carolyn J. Anderson , Thomas P. Quinn
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摘要: Abstract Epidermal growth factor receptor-2 (EGFR-2) has been implicated in the pathogenesis of breast and other carcinomas. In this report, we tested ability a bacteriophage selected peptide KCCYSL, radiolabeled with 64Cu, to image EGFR-2 expressing tumors vivo by positron emission tomography (PET). We evaluated compared tissue distribution imaging properties 64Cu-X-(Gly-Ser-Gly)-KCCYSL (X = 1,4,7,10, tetraazacyclododecane-N,N’,N’’,N’’’-tetracetic acid, [DOTA] 1,4,8,11-tetraazabicyclo[6.6.2]hexadecane-4,11-diacetic acid [CB-TE2A], 1,4,7-triazacyclononane-1,4,7-triacetic [NOTA] chelators) human cancer xenograft mouse model using dual modality PET computed (CT). The synthesized peptides DO3A-GSG-KCCYSL, CB-TE2A-GSG-KCCYSL, NO2A-GSG-KCCYSL were purified, for cell (MDA-MB-435) binding, 50% inhibitory concentration, serum stability. pharmacokinetic s...
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