Applications of glycosyltransferases in the site-specific conjugation of biomolecules and the development of a targeted drug delivery system and contrast agents for MRI.
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.


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.
Ramakrishnan
Boopathy
B
Boeggeman
Elizabeth
E
Qasba
Pradman K
PK
D000818:Animals; D001665:Binding Sites; D003287:Contrast Media / Q000008:administration & dosage / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000379:methods*; D016695:Glycosyltransferases / Q000737:chemistry* / Q000235:genetics; D006801:Humans; D008279:Magnetic Resonance Imaging; D009154:Mutation; D004364:Pharmaceutical Preparations / Q000008:administration & dosage / Q000737:chemistry*
D003287:Contrast Media; D004364:Pharmaceutical Preparations; D016695:Glycosyltransferases