title: Bioconjugation using mutant glycosyltransferases for the site-specific labeling of biomolecules with sugars carrying chemical handles.
abstract: This chapter presents a technique that employs mutant glycosyltransferase enzymes for the site-specific bioconjugation of biomolecules via a glycan moiety to facilitate the development of a targeted drug delivery system. The target specificity of this methodology is based on unique sugar residues that are present on glycoproteins or engineered glycopeptides. The glycosyltransferases used in this approach have been manipulated in a way that confers the ability to transfer a modified sugar residue with a chemical handle to a sugar moiety of the glycoprotein or to a polypeptide tag of an engineered nonglycoprotein. The availability of the modified sugar moiety thus makes it possible to link cargo molecules at specific sites. The cargo may be comprised of, for example, biotin or fluorescent tags for detection, imaging agents for magnetic resonance imaging (MRI), or cytotoxic drugs for cancer therapy.
authors.forename: Boopathy
authors.initials: B
authors.lastname: Ramakrishnan
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Boeggeman
authors.forename: Marta
authors.initials: M
authors.lastname: Pasek
authors.forename: Pradman K
authors.initials: PK
authors.lastname: Qasba
mesh_terms: D001212:Asialoglycoproteins / Q000737:chemistry / Q000378:metabolism; D001665:Binding Sites; D019921:Biotinylation; D050260:Carbohydrate Metabolism; D002846:Chromatography, Affinity; D004337:Drug Carriers / Q000737:chemistry / Q000378:metabolism; D060748:Fetuins; D006023:Glycoproteins / Q000737:chemistry / Q000378:metabolism; D006031:Glycosylation; D016695:Glycosyltransferases / Q000235:genetics* / Q000378:metabolism*; D006801:Humans; D008163:Luminescent Measurements; D013058:Mass Spectrometry; D009154:Mutation; D009844:Oligosaccharides / Q000737:chemistry / Q000378:metabolism; D043524:Peptide-N4-(N-acetyl-beta-glucosaminyl) Asparagine Amidase / Q000378:metabolism; D015202:Protein Engineering; D018719:Erb-b2 Receptor Tyrosine Kinases / Q000276:immunology; D011993:Recombinant Fusion Proteins / Q000276:immunology / Q000378:metabolism; D057127:Single-Chain Antibodies / Q000276:immunology / Q000378:metabolism; D013194:Staining and Labeling / Q000379:methods*; D013205:Staphylococcal Protein A / Q000737:chemistry; D013379:Substrate Specificity; D000509:alpha-Fetoproteins / Q000737:chemistry / Q000378:metabolism
chemical_list: D001212:Asialoglycoproteins; D004337:Drug Carriers; D060748:Fetuins; D006023:Glycoproteins; D016695:Glycosyltransferases; D009844:Oligosaccharides; D043524:Peptide-N4-(N-acetyl-beta-glucosaminyl) Asparagine Amidase; D018719:Erb-b2 Receptor Tyrosine Kinases; D011993:Recombinant Fusion Proteins; D057127:Single-Chain Antibodies; D013205:Staphylococcal Protein A; D000509:alpha-Fetoproteins; C017029:asialofetuin