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.
Melançon
Charles E
CE
Department of Chemistry and Biochemistry, College of Pharmacy, University of Texas at Austin, Austin, Texas 78712, USA.
Thibodeaux
Christopher J
CJ
Liu
Hung-wen
HW
D050260:Carbohydrate Metabolism; D002384:Catalysis; D005947:Glucose / Q000378:metabolism; D006031:Glycosylation; D016695:Glycosyltransferases / Q000378:metabolism
D016695:Glycosyltransferases; D005947:Glucose