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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.