Several glycoprocessing enzymes and glycoreceptors have been recognized as important targets for therapeutic intervention. This concept inspired the development of important classes of therapeutic, such as anti flu drugs inhibiting influenza virus neuraminidase, anti-inflammatory drugs targeting lectin-sialyl-Lewis x interaction and glycosidase inhibitors against HIV, Gaucher’s disease, hepatitis, cancer. These therapeutics are mainly carbohydrate mimics in which proper modifications allow a stronger interaction with the target protein, an higher stability, better pharmacokinetic properties and eventually an 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 review will present examples on how to exploit carbohydrates mimics and scaffolds in drug research.

Cipolla, L., LA FERLA, B., Airoldi, C., Zona, C., Orsato, A., Shaikh, N., et al. (2010). Carbohydrate Mimetics and Scaffolds: Sweet Spots in Medicinal Chemistry. FUTURE MEDICINAL CHEMISTRY, 2(4), 587-599 [10.4155/fmc.10.8].

Carbohydrate Mimetics and Scaffolds: Sweet Spots in Medicinal Chemistry

CIPOLLA, LAURA FRANCESCA;LA FERLA, BARBARA;AIROLDI, CRISTINA;ZONA, CRISTIANO;ORSATO, ALEXANDRE;SHAIKH, NASRIN ISMAIL;RUSSO, LAURA;NICOTRA, FRANCESCO
2010

Abstract

Several glycoprocessing enzymes and glycoreceptors have been recognized as important targets for therapeutic intervention. This concept inspired the development of important classes of therapeutic, such as anti flu drugs inhibiting influenza virus neuraminidase, anti-inflammatory drugs targeting lectin-sialyl-Lewis x interaction and glycosidase inhibitors against HIV, Gaucher’s disease, hepatitis, cancer. These therapeutics are mainly carbohydrate mimics in which proper modifications allow a stronger interaction with the target protein, an higher stability, better pharmacokinetic properties and eventually an 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 review will present examples on how to exploit carbohydrates mimics and scaffolds in drug research.
Articolo in rivista - Articolo scientifico
Glycomimetics, Carbohydrate Scaffolds
English
587
599
13
Cipolla, L., LA FERLA, B., Airoldi, C., Zona, C., Orsato, A., Shaikh, N., et al. (2010). Carbohydrate Mimetics and Scaffolds: Sweet Spots in Medicinal Chemistry. FUTURE MEDICINAL CHEMISTRY, 2(4), 587-599 [10.4155/fmc.10.8].
Cipolla, L; LA FERLA, B; Airoldi, C; Zona, C; Orsato, A; Shaikh, N; Russo, L; Nicotra, F
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10281/16630
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