期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 24, 页码 7513-7515出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.06.107
关键词
Radioimmunotherapy; Bifunctional ligand; (212)Bi; (213)Bi; Trastuzumab
资金
- National Institutes of Health [K22CA102637, R01CA112503]
- NIH, National Cancer Institute, Center for Cancer Research
A new bifunctional ligand C-DEPA was designed and synthesized as a component for antibody-targeted radiation therapy (radioimmunotherapy, RIT) of cancer. C-DEPA was conjugated to a tumor targeting antibody, trastuzumab, and the corresponding C-DEPA-trastuzumab conjugate was evaluated for radiolabeling kinetics with (205/6)Bi. C-DEPA-trastuzumab conjugate rapidly bound (205/6)Bi, and (205/6)Bi-C-DEPA-trastuzumab conjugate was stable in human serum for 72 h. The in vitro radiolabeling kinetics and serum stability data suggest that C-DEPA is a potential chelate for preclinical RIT applications using (212)Bi and (213)Bi. (C) 2011 Published by Elsevier Ltd.
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