Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 26, Issue 19, Pages 5368-5377Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2018.08.036
Keywords
Peptide phage display; Glycopeptides; DC-SIGN
Funding
- Alberta Glycomic Centre
- NSERC [402511]
- Alberta Innovates Technology Futures Graduate Fellowship
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We have employed genetically-encoded fragment-based discovery to identify novel glycopeptides with affinity for the dendritic cell receptor DC-SIGN. Starting from libraries of 10(8) mannose-conjugated peptides, we identified glycopeptides that exhibited up to a 650-fold increase in multivalent binding affinity for DC-SIGN, which is also preserved in cells. Monovalently, our most potent glycopeptides have a similar potency to a Man(3) oligosaccharide, representing a 15-fold increase in activity compared to mannose. These compounds represent the first examples of glycopeptide ligands that target the CRD of DC-SIGN. The natural framework of glycopeptide conjugates and the simplicity of orthogonal conjugation to make these glycopeptides anticipates a promising future for development of DC-SIGN-targeting moieties.
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