期刊
INORGANIC CHEMISTRY
卷 55, 期 14, 页码 6892-6901出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.inorgchem.6b00395
关键词
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资金
- National Institute of Biomedical Imaging and Bioengineering [R21-EB017317]
- Specialized Research Fund for the Doctoral Program of Higher Education of China [20120142120095]
- Fundamental Research Fund for the Central Universities [2016YXMS140, 2014TS090]
- UPCI CCSG [P30CA047904]
Bifunctional chelators play an important role in developing metallic radionuclide-based radiopharmaceuticals. In this study, a new bifunctional ligand, p-SCN-PhPr-NE3TA, was synthesized and conjugated to a very late antigen-4 targeting peptidomimetic, LLP2A, for evaluating its application in Cu-64-based positron emission tomography (PET) imaging. The new ligand exhibited strong selective coordination of Cu(II), leading to a robust Cu complex, even in the presence of 10-fold Fe(III). The LLP2A conjugate of p-SCN-PhPr-NE3TA was prepared and successfully labeled with Cu-64 under mild conditions. The conjugate Cu-64-NE3TA-PEG(4)-LLP2A showed significantly higher specific activity, compared with Cu-64-NOTA-PEG(4)-LLP2A, while maintaining comparable serum stability. Subsequent biodistribution studies and PET imaging in vivo performance and high tumor uptake with low background, chelator for Cu-based radiopharmaceuticals. in mice bearing B16F10 xenografts confirmed its favorable rendering p-SCN-PhPr-NE3TA a promising bifunctional chelator for Cu-64-based radiopharmaceuticals.
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