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A novel bifunctional maleimido CHX-A'' chelator for conjugation to thiol-containing biomolecules.


ABSTRACT: A novel bifunctional maleimido CHX-A'' DTPA chelator 5 was developed and conjugated to the monoclonal antibody trastuzumab (Herceptin) and subsequently radiolabeled with (111)In. The resulting (111)In labeled immunoconjugate 2 was demonstrated to bind to SKOV-3 ovarian cancer cells comparably to an isothiocyanato CHX-A'' DTPA modified native trastuzumab, 1. Through efficient thiol-maleimide chemistry, antibodies, peptides or other targeting vectors can now be modified with an established radioactive metal chelating agent CHX-A'' DTPA for imaging and/or therapies of cancer.

SUBMITTER: Xu H 

PROVIDER: S-EPMC2346453 | biostudies-literature | 2008 Apr

REPOSITORIES: biostudies-literature

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A novel bifunctional maleimido CHX-A'' chelator for conjugation to thiol-containing biomolecules.

Xu Heng H   Baidoo Kwamena E KE   Wong Karen J KJ   Brechbiel Martin W MW  

Bioorganic & medicinal chemistry letters 20080310 8


A novel bifunctional maleimido CHX-A'' DTPA chelator 5 was developed and conjugated to the monoclonal antibody trastuzumab (Herceptin) and subsequently radiolabeled with (111)In. The resulting (111)In labeled immunoconjugate 2 was demonstrated to bind to SKOV-3 ovarian cancer cells comparably to an isothiocyanato CHX-A'' DTPA modified native trastuzumab, 1. Through efficient thiol-maleimide chemistry, antibodies, peptides or other targeting vectors can now be modified with an established radioac  ...[more]

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