title: Carbohydrate mimetics and scaffolds: sweet spots in medicinal chemistry.
abstract: Several glycoprocessing enzymes and glycoreceptors have been recognized as important targets for therapeutic intervention. This concept has inspired the development of important classes of therapeutics, such as anti-influenza drugs inhibiting influenza virus neuraminidase, anti-inflammatory drugs targeting lectin-sialyl-Lewis X interaction and glycosidase inhibitors against HIV, Gaucher's disease, hepatitis and cancer. These therapeutics are mainly carbohydrate mimics in which proper modifications permit stronger interactions with the target protein, higher stability, better pharmacokinetic properties and easier synthesis. Furthermore, the conformational rigidity and polyfunctionality of carbohydrates stimulate their use as scaffolds for the generation of libraries by combinatorial decoration with different pharmacophores. This mini-review will present examples of how to exploit carbohydrates mimics and scaffolds in drug research.
authors.affiliation: Department of Biotechnology and Biosciences, University of Milano-Biococca, Piazza della Scienza 2, I-20126 Milano, Italy. francesco.nicotra@unimib.it
authors.forename: Laura
authors.initials: L
authors.lastname: Cipolla
authors.forename: Barbara
authors.initials: B
authors.lastname: La Ferla
authors.forename: Cristina
authors.initials: C
authors.lastname: Airoldi
authors.forename: Cristiano
authors.initials: C
authors.lastname: Zona
authors.forename: Alexandre
authors.initials: A
authors.lastname: Orsato
authors.forename: Nasrin
authors.initials: N
authors.lastname: Shaikh
authors.forename: Laura
authors.initials: L
authors.lastname: Russo
authors.forename: Francesco
authors.initials: F
authors.lastname: Nicotra
mesh_terms: D002236:Carbohydrate Conformation; D002240:Carbohydrate Sequence; D002241:Carbohydrates / Q000737:chemistry* / Q000627:therapeutic use*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D006801:Humans; D018716:Molecular Mimicry; D008969:Molecular Sequence Data; D015394:Molecular Structure; D009584:Nitrogen / Q000737:chemistry; D010100:Oxygen / Q000737:chemistry
chemical_list: D002241:Carbohydrates; D009584:Nitrogen; D010100:Oxygen