BACKGROUND: The delivery of drugs to the proposed site of action is a challenging task. Tissue and cell-specific guiding molecules are being used to carry a cargo of therapeutic molecules. The cargo molecules need to be conjugated in a site-specific manner to the therapeutic molecules such that the bioefficacy of these molecules is not compromised. METHODS: Using wild-type and mutant glycosyltransferases, the sugar moiety with a unique chemical handle is incorporated at a specific site in the cargo or therapeutic molecules, making it possible to conjugate these molecules through the chemical handle present on the modified glycan. RESULTS/ CONCLUSIONS: The modified glycan residues introduced at specific sites on the cargo molecule make it possible to conjugate fluorophores for ELISA-based assays, radionuclides for imaging and immunotherapy applications, lipids for the assembly of immunoliposomes, cytotoxic drugs, cytokines, or toxins for antibody-based cancer therapy and the development of a targeted drug delivery system.
BACKGROUND: The delivery of drugs to the proposed site of action is a challenging task. Tissue and cell-specific guiding molecules are being used to carry a cargo of therapeutic molecules. The cargo molecules need to be conjugated in a site-specific manner to the therapeutic molecules such that the bioefficacy of these molecules is not compromised. METHODS: Using wild-type and mutant glycosyltransferases, the sugar moiety with a unique chemical handle is incorporated at a specific site in the cargo or therapeutic molecules, making it possible to conjugate these molecules through the chemical handle present on the modified glycan. RESULTS/ CONCLUSIONS: The modified glycan residues introduced at specific sites on the cargo molecule make it possible to conjugate fluorophores for ELISA-based assays, radionuclides for imaging and immunotherapy applications, lipids for the assembly of immunoliposomes, cytotoxic drugs, cytokines, or toxins for antibody-based cancer therapy and the development of a targeted drug delivery system.
Authors: Nelly Khidekel; Sabine Arndt; Nathan Lamarre-Vincent; Alexander Lippert; Katherine G Poulin-Kerstien; Boopathy Ramakrishnan; Pradman K Qasba; Linda C Hsieh-Wilson Journal: J Am Chem Soc Date: 2003-12-31 Impact factor: 15.419
Authors: Elizabeth Boeggeman; Boopathy Ramakrishnan; Marta Pasek; Maria Manzoni; Anu Puri; Kristin H Loomis; Timothy J Waybright; Pradman K Qasba Journal: Bioconjug Chem Date: 2009-06 Impact factor: 4.774
Authors: Hendrik Schneider; Lukas Deweid; Thomas Pirzer; Desislava Yanakieva; Simon Englert; Bastian Becker; Olga Avrutina; Harald Kolmar Journal: ChemistryOpen Date: 2019-03-28 Impact factor: 2.911