Smith RA, Yuan H, Weissleder R, Cantley LC, Josephson L
A Wortmannin-Cetuximab as a Double Drug. [JOURNAL ARTICLE]
Bioconjug Chem 2009 Nov 2.
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.
More from this journal |
