Glyco-stripping and glyco-swapping.

Glycosyltransferases (GTs) are ubiquitous enzymes that catalyze the transfer of a sugar moiety from an activated donor to an acceptor and thus play important roles in natural product biogenesis, virulence, and biomolecular recognition. Sugars are often critical for bioactivity of natural products, and methodologies for creating diverse glycoforms of these compounds are highly desirable. A recent study demonstrates that several GTs involved in natural product biosynthesis catalyze reversible reactions. Sugar exchange and aglycon exchange strategies were used to exploit this reversibility to generate >70 calicheamicin analogues.