Acceptor substrate-based selective inhibition of galactosyltransferases

This paper describes the discovery of glycosyl acceptor analogs as potent a nd selective inhibitors of alpha-1,3- and beta-1,4-galactosyltransferases. Incorporation of an appropriate aromatic group to the aglycon position of t he enzyme's accepters results in a strong inhibition, representing the firs t and most potent small uncharged molecules as selective inhibitors of thes e two enzymes and thus providing a new strategy for the development of sele ctive glycosyltransferase inhibitors. (C) 1998 Published by Elsevier Scienc e Ltd. All rights reserved.