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