Naturally occurring glycopeptides (GPs, peptide + sugar) and glycoproteins are crucial players in many biological processes. N- and O-glycosylation is in fact one of the most important post-translational modifications in vivo. Glycoproteins are fundamental in cell-cell communications, recognition of viruses and bacteria by host cells, and tumor progression. Therefore, GPs can be used for emulating glycoprotein epitopes, and as such are recognized as important conjugates for immunostimulation and vaccines. In the drug discovery field, the attachment of carbohydrates to bioactive peptides can also serve to improve pharmacological properties (binding affinity and/or potency), to enhance metabolic stability, to modify biodistribution (targeted delivery), and to increase penetration across biological membranes.

This short compendium covers recent advancements in the continuously evolving GP field, describing a selection of representative examples of glycopeptides acting as antibiotics, HIV and cancer immunogens, protein-protein inhibitors and improved central nervous system agents.

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Contributed by Rosario González-Muñiz

Rosario is a Senior Researcher at the Medicinal Chemistry Institute (IQM-CSIC), Madrid. She is involved in peptides, secondary structure mimics and small-molecule peptidomimetics of application in biological/medicinal chemistry programs, especially related to the modulation of ion channels and associated proteins.