A novel bifunctional maleimido CHX-A' chelator for conjugation to thiol-containing biomolecules |
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Authors: | Xu Heng Baidoo Kwamena E Wong Karen J Brechbiel Martin W |
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Institution: | Radioimmune & Inorganic Chemistry Section, Radiation Oncology Branch, National Cancer Institute, National Institutes of Health, Building 10, Room 1B40, 10 Center Drive, Bethesda, MD 20892-1088, USA. |
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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. |
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