Acceptor substrate-based selective inhibition of galactosyltransferases

This paper describes the discovery of glycosyl acceptor analogs as potent and selective inhibitors of α-1,3- and β-1,4-galactosyltransferases. Incorporation of an appropriate aromatic group to the aglycon position of the enzymeʹs acceptors results in a strong inhibition, representing the first and most potent small uncharged molecules as selective inhibitors of these two enzymes and thus providing a new strategy for the development of selective glycosyltransferase inhibitors.