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high in vivo stability of 64 cu-labeled cross-bridged chelators is a crucial factor in improved tumor imaging of rgd peptide conjugates
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نویسنده
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sarkar s. ,bhatt n. ,ha y.s. ,huynh p.t. ,soni n. ,lee w. ,lee y.j. ,kim j.y. ,pandya d.n. ,an g.i. ,lee k.c. ,chang y. ,yoo j.
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منبع
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journal of medicinal chemistry - 2018 - دوره : 61 - شماره : 1 - صفحه:385 -395
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چکیده
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Although the importance of bifunctional chelators (bfcs) is well recognized, the chemophysical parameters of chelators that govern the biological behavior of the corresponding bioconjugates have not been clearly elucidated. here, five bfcs closely related in structure were conjugated with a cyclic rgd peptide and radiolabeled with cu-64 ions. various biophysical and chemical properties of the cu(ii) complexes were analyzed with the aim of identifying correlations between individual factors and the biological behavior of the conjugates. tumor uptake and body clearance of the 64 cu-labeled bioconjugates were directly compared by animal pet imaging in animal models, which was further supported by biodistribution studies. conjugates containing propylene cross-bridged chelators showed higher tumor uptake, while a closely related ethylene cross-bridged analogue exhibited rapid body clearance. high in vivo stability of the copper-chelator complex was strongly correlated with high tumor uptake, while the overall lipophilicity of the bioconjugate affected both tumor uptake and body clearance.
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آدرس
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kyungpook national university, department of molecular medicine, bk21 plus knu biomedical convergence program, south korea, kyungpook national university, department of molecular medicine, bk21 plus knu biomedical convergence program, south korea, kyungpook national university, department of molecular medicine, bk21 plus knu biomedical convergence program, south korea, kyungpook national university, department of molecular medicine, bk21 plus knu biomedical convergence program, south korea, kyungpook national university, department of molecular medicine, bk21 plus knu biomedical convergence program, south korea, kyungpook national university, department of molecular medicine, bk21 plus knu biomedical convergence program, south korea, korea institute of radiological and medical sciences, department of ri-convergence research, south korea, korea institute of radiological and medical sciences, department of ri-convergence research, south korea, kyungpook national university, department of molecular medicine, bk21 plus knu biomedical convergence program, south korea, korea institute of radiological and medical sciences, department of ri-convergence research, south korea, korea institute of radiological and medical sciences, department of ri-convergence research, south korea, kyungpook national university, department of molecular medicine, bk21 plus knu biomedical convergence program, south korea, kyungpook national university, department of molecular medicine, bk21 plus knu biomedical convergence program, south korea
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Authors
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