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.
Publication types
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Research Support, N.I.H., Intramural
MeSH terms
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Antibodies, Monoclonal / chemistry
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Antibodies, Monoclonal / immunology
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Antibodies, Monoclonal, Humanized
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Cell Line, Tumor
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Chelating Agents / chemical synthesis
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Chelating Agents / chemistry*
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Chromatography, High Pressure Liquid
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Humans
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Isothiocyanates / chemical synthesis
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Isothiocyanates / chemistry*
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Maleimides / chemistry*
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Molecular Structure
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Pentetic Acid / analogs & derivatives*
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Pentetic Acid / chemical synthesis
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Pentetic Acid / chemistry
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Sulfhydryl Compounds / chemistry*
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Sulfhydryl Compounds / metabolism*
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Trastuzumab
Substances
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Antibodies, Monoclonal
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Antibodies, Monoclonal, Humanized
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Chelating Agents
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Isothiocyanates
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Maleimides
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Sulfhydryl Compounds
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N-(2-amino-3-(4-isothiocyanatophenyl)propyl)cyclohexane-1,2-diamine-N,N',N',N'',N''-pentaacetic acid
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maleimide
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Pentetic Acid
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Trastuzumab