RSC_Chemical Science

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14 September 2019 

Issue 34

Page 7825 to 8048 




Biomedical applications of copper-free click chemistry: in vitro, in vivo, and ex vivo


Recently, click chemistry has provided important advances in biomedical research fields. Particularly, copper-free click chemistry including strain-promoted azide–alkyne cycloaddition (SPAAC) and inverse-electron-demand Diels–Alder (iEDDA) reactions enable fast and specific chemical conjugation under aqueous conditions without the need for toxic catalysts. Click chemistry has resulted in a change of paradigm, showing that artificial chemical reactions can occur on cell surfaces, in cell cytosol, or within the body, which is not easy with most other chemical reactions. Click chemistry in vitro allows specific labelling of cellular target proteins and studying of drug target engagement with drug surrogates in live cells. Furthermore, cellular membrane lipids and proteins could be selectively labelled with click chemistry in vitro and cells could be adhered together using click chemistry. Click chemistry in vivo enables efficient and effective molecular imaging and drug delivery for diagnosis and therapy. 





  • Eunha Kim
  • Heebeom Koo

 


https://pubs.rsc.org/en/content/articlelanding/2019/sc/c9sc90186h#!divAbstract



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