It has been shown that all selectins recognize the carbohydrate epitopes si
alyl Lewis(x) and sialyl Lewis(a). For the establishment of the structure-a
ctivity relationship, the efficient synthesis of these tetrasaccharides and
derivatives is therefore of vital interest. The glycosyl transferase-media
ted approach is summarized with emphasis on the use of modified acceptors a
nd modified sugar-nucleotide donors. A survey of the involved enzymes: beta
(1-3) and beta(1-4)galactosyl transferases, alpha(2-3)sialyl transferase, F
ucT III and FucT VI reveals that the enzymatic synthesis is highly efficien
t for the rapid preparation of sialyl Lewis(x)- and sialyl Lewis(a)-derivat
ives.