Enhancing the anticancer properties of cardiac glycosides by neoglycorandomization

Joseph M. Langenhan, Noël R. Peters, Ilia A. Guzei, F. Michael Hoffmann, Jon S. Thorson

Research output: Contribution to journalArticlepeer-review

213 Scopus citations


Glycosylated natural products are reliable platforms for the development of many front-line drugs, yet our understanding of the relationship between attached sugars and biological activity is limited by the availability of convenient glycosylation methods. When a universal chemical glycosylation method that employs reducing sugars and requires no protection or activation is used, the glycorandomization of digitoxin leads to analogs that display significantly enhanced potency and tumor specificity and suggests a divergent mechanistic relationship between cardiac glycoside-induced cytotoxicity and Na +/K+-ATPase inhibition. This report highlights the remarkable advantages of glycorandomization as a powerful tool in glycobiology and drug discovery.

Original languageEnglish
Pages (from-to)12305-12310
Number of pages6
JournalProceedings of the National Academy of Sciences of the United States of America
Issue number35
StatePublished - Aug 30 2005


  • Carbohydrate
  • Natural product
  • Sugar

ASJC Scopus subject areas

  • General


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