Enzymatic methods for glyco(diversification/randomization) of drugs and small molecules

Richard W. Gantt, Pauline Peltier-Pain, Jon S. Thorson

Research output: Contribution to journalReview articlepeer-review

216 Scopus citations


Covering: up to the end of May 2011 Glyco(randomization/diversification) is a term that encompasses strategies to diversify a core drug scaffold via enzymatic glycosylation to provide sets of analogs wherein the sole diversity element is a carbohydrate. This review covers the influence of glycosylation upon various drug properties, the classes of glycosyl-conjugating enzymes amenable to glyco(randomization/diversification) schemes, approaches to the synthesis of required substrates and specific examples of glycorandomized libraries utilizing both wild-type and engineered enzymes.

Original languageEnglish
Pages (from-to)1811-1853
Number of pages43
JournalNatural Product Reports
Issue number11
StatePublished - Nov 2011

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry


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