- Bioconjugation by native chemical tagging of C-H bonds.
Bioconjugation by native chemical tagging of C-H bonds.
Journal of the American Chemical Society (2013-08-21)
Qianghui Zhou, Jinghan Gui, Chung-Mao Pan, Earl Albone, Xin Cheng, Edward M Suh, Luigi Grasso, Yoshihiro Ishihara, Phil S Baran
PMID23957305
RÉSUMÉ
A general C-H functionalization method for the tagging of natural products and pharmaceuticals is described. An azide-containing sulfinate reagent allows the appendage of azidoalkyl chains onto heteroaromatics, the product of which can then be attached to a monoclonal antibody by a "click" reaction. This strategy expands the breadth of bioactive small molecules that can be linked to macromolecules in a manner that is beyond the scope of existing methods in bioconjugation to permit tagging of the "seemingly untaggable".
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