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Synthesis and preclinical characterization of [64Cu]NODAGA-MAL-exendin-4 with a Nε-maleoyl-L-lysyl-glycine linkage.

Nucl. Med. Biol.. 2013; 
YimCheng-Bin,MikkolaKirsi,FagerholmVeronica,ElomaaViki-Veikko,IshizuTamiko,RajanderJohan,SchlesingerJoern,RoivainenAnne,NuutilaPirjo,Solin
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Proteins, Expression, Isolation and Analysis … NODAGA-tris( t Bu) (4-(4,7-bis(2-(tert-butoxy)-2-oxoethyl)-1,4,7-triazacyclononan-1-yl)- 5-(tert-butoxy)-5-oxopentanoic acid) was purchased from CheMatech (Dijon, France). [ 40 Cys]exendin-4(1-39) was purchased from GenScript USA Inc … Get A Quote

摘要

Renal localization of high radioactivity levels during targeted imaging compromises tissue visualization in the kidney region and limits diagnostic accuracy. Radioiodinated antibody fragments with a renal enzyme-cleavable N(ε)-maleoyl-L-lysyl-glycine (MAL) linkage demonstrated low renal radioactivity levels in mice, from early postinjection times. This study tested the hypothesis whether a (64)Cu-labeled NODAGA-exendin-4 peptide with a MAL linkage ([(64)Cu]NODAGA-MAL-exendin-4) could decrease kidney radioactivity levels in rats, compared to a [(64)Cu]NODAGA-exendin-4 reference, without impairing the radioactivity levels in the target tissue.

关键词

Copper-64,Exendin,GLP-1 receptor,NODAGA,Renal brush border memb