Drug discovery has long suffered from the difficulty of having to place pharmacophoric groups in just the right spatial arrangement to elicit the desired biological response Although some molecule classes have been discovered that seem to be privileged structures for at least some drug-receptor interactions, there remains the challenge to design and synthesize molecules with high specific affinity to pharmacologically important targets With their high density of stereochemical information and their relative rigidity, carbohydrates provide excellent platforms upon which to display a number of substituents in a sterically defined way, hence offering the opportunity to harness their unique features for the drug-discovery process This review highlights the progress that has been made in the development of carbohydrate scaffolds for drug discovery

Carbohydrates as Scaffolds in Drug Discovery

Molecular diversity through sugar scaffolds.

Importance of the field: Till now, the importance of carbohydrates has been underscored, if compared with the two other major classes of biopolymers such as oligonucleotides and proteins. Recent advances in glycobiology and glycochemistry have imparted a strong interest in the study of this enormous family of biomolecules. Carbohydrates have been shown to be implicated in recognition processes, such as cell–cell adhesion, cell–extracellular matrix adhesion and cell–intruder recognition phenomena. In addition, carbohydrates are recognized as differentiation markers and as antigenic determinants. Due to their relevant biological role, carbohydrates are promising candidates for drug design and disease treatment. However, the growing number of human disorders known as congenital disorders of glycosylation that are being identified as resulting from abnormalities in glycan structures and protein glycosylation strongly indicates that a fast development of glycobiology, glycochemistry and glycomedicine is highly...

Sabrina Giannini

Papers

Design, synthesis and biological activity of carbohydrate-Containing peptidomimetics as new ligands for the human tachykinin NK-2 receptor

Design, Synthesis and Biological Activity of Carbohydrate‐Containing Peptidomimetics as New Ligands for the Human Tachykinin NK‐2 Receptor.