| Title | A Wortmannin-Cetuximab as a Double Drug. | | Author(s) | Smith RA, Yuan H, Weissleder R, Cantley LC, Josephson L | | Institution | Center for Molecular Imaging Research, Massachusetts General Hospital and Harvard Medical School, 149 13th Street, Charlestown, Massachusetts 02129, Center for Systems Biology, Massachusetts General Hospital, Boston, Massachusetts 02114, and Department of Systems Biology, Harvard Medical School and Division of Signal Transduction, Beth Israel Deaconess Medical Center, 77 Avenue Louis Pasteur, Boston Massachusetts 02115. | | Source | Bioconjug Chem 2009 Nov 2. | | Abstract | Double drugs are obtained when two pharmacologically active entities are covalently joined to improve potency. We conjugated the viridin Wm with a self-activating linkage to cetuximab and demonstrated the retention of immunoreactivity by the conjugate. Though cetuximab lacked a growth inhibitory activity against A549 cells, the Wm-cetuximab conjugate had an antiproliferative IC(50) of 155 nM in vitro. The chemistry of attaching a self-releasing Wm to clinically approved antibodies is general and, in selected instances, may yield antibody-based double drugs with improved efficacy. | | Language | ENG | | Pub Type(s) | JOURNAL ARTICLE
| | PubMed ID | 19883074 |
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