Bioconjugation by Native Chemical Tagging of C鈥揌 Bonds
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- 作者：Qianghui Zhou ; Jinghan Gui ; Chung-Mao Pan ; Earl Albone ; Xin Cheng ; Edward M. Suh ; Luigi Grasso ; Yoshihiro Ishihara ; Phil S. Baran
- 刊名：Journal of the American Chemical Society
- 出版年：2013
- 出版时间：September 4, 2013
- 年：2013
- 卷：135
- 期：35
- 页码：12994-12997
- 全文大小：485K
- 年卷期：v.135,no.35(September 4, 2013)
- ISSN：1520-5126
文摘
A general C鈥揌 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 鈥渃lick鈥?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 鈥渟eemingly untaggable鈥?