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.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3741339 | PMC |
| http://dx.doi.org/10.1016/j.bmcl.2011.06.107 | DOI Listing |
Publication Analysis
Top Keywords
c-depa-trastuzumab conjugate
8
radiolabeling kinetics
8
synthesis evaluation
4
evaluation bifunctional
4
bifunctional chelate
4
chelate development
4
development biiii-labeled
4
biiii-labeled radioimmunoconjugates
4
radioimmunoconjugates bifunctional
4
bifunctional ligand
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!