Method of producing 6-thio-sialylated glycoproteins and glycoconjugates

摘要

The present invention relates to a method of preparing 6-thio-sialyl-glycosyl compounds, comprising the step consisting of reacting in vitro or in vivo 6-thio-sialic acid compounds with a CMP-sialic synthetase to form CMP-6-thio sialic acid compounds and with a sialyltransferase to transfer said CMP-6-thio sialic acid compounds as donor substrate to glycosyl compounds as acceptor subtrate leading to the enzymatic coupling of 6-thiosialic acid compounds onto glycosyl compounds. Glycosyl compounds are selected from glycoproteins, glycolipids and oligosaccharides, including monoclonal antibodies.