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. 2006 Mar 24;8(1):E190–E195. doi: 10.1208/aapsj080123

Mutant glycosyltransferases assist in the development of a targeted drug delivery system and contrast agents for MRI

Pradman K Qasba 2,✉, Boopathy Ramakrishnan 2,1, Elizabeth Boeggeman 2,1
PMCID: PMC2751439  PMID: 16584127

Abstract

The availability of structural information on glycosyltransferases is beginning to make structure-based reengineering of these enzymes possible. Mutant glycosyltransferases have been generated that can transfer a sugar residue with a chemically reactive unique functional group to a sugar moiety of glycoproteins, glycolipids, and proteoglycans (glyco-conjugates). The presence of modified sugar moiety on a glycoprotein makes it possible to link bioactive molecules via modified glycan chains, thereby assisting in the assembly of bionanoparticles that are useful for developing the targeted drug delivery system and contrast agents for magnetic resonance imaging. The reengineered recombinant glycosyltransferases also make it possible to (1) remodel the oligosaccharide chains of glycoprotein drugs, and (2) synthesize oligosaccharides for vaccine development.

Keywords: mutant glycosyltransferases, linkages via glycans, glycotargeting, drug delivery systems, cross-linking MRI agents via glycans

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