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Rek, A; Krenn, E; Kungl, AJ.
Therapeutically targeting protein-glycan interactions.
Br J Pharmacol. 2009; 157(5): 686-94. Doi: 10.1111/j.1476-5381.2009.00226.x [OPEN ACCESS]
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Co-Autor*innen der Med Uni Graz
Jantscher-Krenn Evelyn
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Abstract:
Glycosylation is the most common form of post-translational modifications by which oligosaccharide side chains are covalently attached to specific residues of the core protein. Especially O-linked glycan structures like the glycosaminoglycans were found to contribute significantly to many (patho-)biological processes like inflammation, coagulation, cancer and viral infections. Glycans exert their function by interacting with proteins thereby changing the structure of the interacting proteins and consequently modulating their function. Given the complex nature of cell-surface and extracellular matrix glycan structures, this therapeutic site has been neglected for a long time, the only exception being the antithrombin III-glycan interaction which has been successfully targeted by unfractionated and low-molecular weight heparins for many decades. Due to the recent breakthrough in the '-ome' sciences, among them proteomics and glycomics, protein-glycan interactions became more amenable for therapeutic approaches so that novel inhibitors of this interaction are currently in preclinical and clinical studies. An overview of current approaches, their advantages and disadvantages, is given and the promising potential of pharmacologically interfering with protein-glycan interactions is highlighted here.
Find related publications in this database (using NLM MeSH Indexing)
Animals - administration & dosage
Binding Sites - administration & dosage
Carbohydrate Conformation - administration & dosage
Drug Design - administration & dosage
Glycomics - methods
Glycosaminoglycans - antagonists & inhibitors, metabolism
Glycosylation - administration & dosage
Heparin - analogs & derivatives, biosynthesis
Humans - administration & dosage
Ligands - administration & dosage
Models, Molecular - administration & dosage
Molecular Structure - administration & dosage
Protein Conformation - administration & dosage
Protein Processing, Post-Translational - drug effects
Proteoglycans - biosynthesis, chemistry, drug effects
Proteomics - methods
Signal Transduction - drug effects
Structure-Activity Relationship - administration & dosage

Find related publications in this database (Keywords)
glycosaminoglycan
chemokine
growth factor
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