Chemical tumor-targeting of nanoparticles based on metabolic glycoengineering and click chemistry

Sangmin Lee, Heebeom Koo, Jin Hee Na, Seung Jin Han, Hyun Su Min, So Jin Lee, Sun Hwa Kim, Seok Hyun Yun, Seo Young Jeong, Ick Chan Kwon, Kuiwon Choi, Kwangmeyung Kim

Research output: Contribution to journalArticlepeer-review

158 Scopus citations


Tumor-targeting strategies for nanoparticles have been predominantly based on optimization of physical properties or conjugation with biological ligands. However, their tumor-targeting abilities remain limited and insufficient. Furthermore, traditional biological binding molecules have intrinsic limitations originating from the limited amount of cellular receptors and the heterogeneity of tumor cells. Our two-step in vivo tumor-targeting strategy for nanoparticles is based on metabolic glycoengineering and click chemistry. First, an intravenous injection of precursor-loaded glycol chitosan nanoparticles generates azide groups on tumor tissue specifically by the enhanced permeation and retention (EPR) effect followed by metabolic glycoengineering. These 'receptor-like' chemical groups then enhance the tumor-targeting ability of drug-containing nanoparticles by copper-free click chemistry in vivo during a second intravenous injection. The advantage of this protocol over traditional binding molecules is that there are significantly more binding molecules on the surface of most tumor cells regardless of cell type. The subsequent enhanced tumor-targeting ability can significantly enhance the cancer therapeutic efficacy in animal studies.

Original languageEnglish
Pages (from-to)2048-2063
Number of pages16
JournalACS Nano
Issue number3
StatePublished - 25 Mar 2014


  • click chemistry
  • drug delivery
  • metabolic glycoengineering
  • nanoparticle
  • tumor-targeting


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