title: Discovery and design of carbohydrate-based therapeutics.
abstract: BACKGROUND
  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 desirable.
  
  
  METHODS
  The topics give an overview of different approaches that have been used to date for the design of carbohydrate-based therapeutics; this includes the use of native synthetic carbohydrates, the use of carbohydrate mimics designed on the basis of their native counterpart, the use of carbohydrates as scaffolds and finally the design of glyco-fused therapeutics, one of the most recent approaches. The review covers mainly literature that has appeared since 2000, except for a few papers cited for historical reasons.
  
  
  RESULTS
  The reader will gain an overview of the current strategies applied to the design of carbohydrate-based therapeutics; in particular, the advantages/disadvantages of different approaches are highlighted. The topic is presented in a general, basic manner and will hopefully be a useful resource for all readers who are not familiar with it. In addition, in order to stress the potentialities of carbohydrates, several examples of carbohydrate-based marketed therapeutics are given.
  
  
  CONCLUSIONS
  Carbohydrates are a rich class of natural compounds, possessing an intriguing and still not fully understood biological role. This richness offers several strategies for the design of carbohydrate-based therapeutics.
authors: University of Milano-Bicocca, Department of Biotechnology and Biosciences, Piazza della Scienza 2, 20126 Milano, Italy. laura.cipolla@unimib.it
authors: Laura
authors: L
authors: Cipolla
authors: Ana C
authors: AC
authors: Araújo
authors: Davide
authors: D
authors: Bini
authors: Luca
authors: L
authors: Gabrielli
authors: Laura
authors: L
authors: Russo
authors: Nasrin
authors: N
authors: Shaikh
mesh_terms: D000818:Animals; D001428:Bacterial Vaccines; D002236:Carbohydrate Conformation; D002241:Carbohydrates / Q000737:chemistry* / Q000276:immunology*; D015195:Drug Design; D013329:Structure-Activity Relationship
chemical_list: D001428:Bacterial Vaccines; D002241:Carbohydrates