Serum stability of 67Cu chelates: Comparison with 111In and 57Co☆
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Imaging, biodistribution and in vitro study of smart <sup>99m</sup>Tc-PAMAM G4 dendrimer as novel nano-complex
2017, Colloids and Surfaces B: BiointerfacesCitation Excerpt :In comparison with antibody labeling efficiency, PAMAM G4 nanoparticle could be considered as good candidate for radiolabeling and imaging [41]. In general, stability decreases after 24 h which could be attributed to protein interactions such as albumin in the serum [42]. Cellular uptake of FA targeted nano-carrier was evaluated on normal and cancer cell lines to investigate FR-mediated endocytosis (Fig. 4C and D).
Development of [<sup>64</sup>Cu]-DOTA-PR81 radioimmunoconjugate for MUC-1 positive PET imaging
2016, Nuclear Medicine and BiologyCitation Excerpt :The results showed that after incubation of 64Cu-DOTA-PR81 (300 μCi) with freshly prepared human serum at 37 °C for up to 48 h, more than 78% of total radioactivity was eluted in the same position as 64Cu-DOTA-PR81. Cole et al. reported that decreases of stability in human serum resulted from mild trans-chelation of 64Cu to serum components such as albumin [31], while Cooper et al. reported the high stability of macrocyclic immunoconjugates such as DOTA-mAb, DO3A-mAb and NOTA-mAb in serum over 48 h [32]. These data are in agreement with our data.
Transferrin conjugates of triazacyclononane-based bifunctional NE3TA chelates for PET imaging: Synthesis, Cu-64 radiolabeling, and in vitro and in vivo evaluation
2016, Journal of Inorganic BiochemistryCitation Excerpt :The Student t-test was used to determine significance at the 95% confidence level and P values of < 0.05 were considered significantly different. Introduction of a functional unit to the chelate backbone is known to affect stability and formation rate of metal complexes [10,17–19]. The three different bifunctional ligands N-NE3TA, C-NE3TA, and C-NE3TA–Bn (7-[2-[(carboxymethyl)amino]-2-(phenylmethyl)]-3-(4-nitrophenyl)propyl]-1,4,7-triazacyclononane-1,4-diacetic acid), containing the isothiocyanate (NCS) group for conjugation to transferrin, were prepared and evaluated in an effort to identify the best bifunctional version.
Copper-64 radiolabeling and biological evaluation of bifunctional chelators for radiopharmaceutical development
2012, Nuclear Medicine and BiologyCitation Excerpt :Earliest reported BFCs were derived from well established non-macrocyclic chelating agents e.g. ethylenediamine tetraacetic acid (EDTA). However, Cu complexes of non-macrocyclic chelators such as EDTA and diethylenetriamine pentaacetic acid (DTPA) have been shown to be unstable in vivo although the complexes are thermodynamically stable [5,6]. In response to the kinetic instability of acyclic chelators, macrocyclic BFC derivatives of 1,4,7,10-tetra-azacylcododecane-N,N′,N″,N′″-tetraacetic acid (DOTA) and 1,4,8,11-tetraazacyclotetra decane-N,N′,N″,N′″-tetraacetic acid (TETA) derivatives have been developed for complexing with 64Cu.
Imaging cancer using PET - the effect of the bifunctional chelator on the biodistribution of a 64Cu-labeled antibody
2011, Nuclear Medicine and BiologyCitation Excerpt :However, the kinetic stability of the metal complex, the rate at which the metal is lost from the ligand, the effect of in vivo chelators, and pH are perhaps more important when considering the stability of the complex in a biological environment. The observation that kinetic stability is of paramount importance in radiometal labeling a biological molecule has been made before [25,27,28]. The BFCs used in this study vary in their properties (e.g., thermodynamic stability, charge, lipophilicity).
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Supported by the U.S. Department of Energy AT03-82 and the National Cancer Institute CA16861.
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Present address: Department of Nuclear Medicine, The Methodist Hospital/Baylor College of Medicine, Houston, Texas, U.S.A.