Synthesis and evaluation of a bifunctional chelate for development of Bi(III)-labeled radioimmunoconjugates.
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ABSTRACT:
SUBMITTER: Dadwal M
PROVIDER: S-EPMC3741339 | biostudies-literature | 2011 Dec
REPOSITORIES: biostudies-literature
Publications
Synthesis and evaluation of a bifunctional chelate for development of Bi(III)-labeled radioimmunoconjugates.
Dadwal Mamta M Kang Chi Soo CS Song Hyun A HA Sun Xiang X Dai Anzhi A Baidoo Kwamena E KE Brechbiel Martin W MW Chong Hyun-Soon HS
Bioorganic & medicinal chemistry letters 20110707 24
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 ...[more]
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