In search for novel drug targets aimed to control CF lung infections, a key role of the non-lysosomal glucosidase 2 (GBA2-encoded GNLase) in proinflammatory state characterizing CF cells has been highlighted. As matter of fact, Miglustat® (d-NBDNJ) has been found to reduce the inflammatory response in P. aeruginosa infected CF bronchial cells showing a therapeutic potential of iminosugars in CF lung disease treatment. However, pharmacological use of d-iminosugars is hampered by their poor in vivo selectivity. Conversely, their non-superimposable mirror image, L-iminosugars have shown higher selectivity acting as inhibitors or enhancers of glycosidases and glycosyltransferases
N-Alkylated L-Iminosugars as novel anti-inflammatory and anti-biofilm tools for Cystic Fibrosis Lung Infections / Esposito, A., DE FENZA, M., D'Alonzo, D., DE GREGORIO, E., Rocco, L., Munari, S., Loberto, N., Santangelo, A., Tamanini, A., Rossi, A., Romanucci, S., De Fino, I., Baragonzi, A., Aureli, M., Lippi, G., De Checchi, M.C., Guaragna, A.. - (2019). (6th EFMC Young Medicinal Chemist Symposium, Athene, Greece 5-6 settembre 2019).
N-Alkylated L-Iminosugars as novel anti-inflammatory and anti-biofilm tools for Cystic Fibrosis Lung Infections
Esposito Anna;De Fenza Maria;D’Alonzo Daniele;De Gregorio Eliana;Guaragna, A
2019
Abstract
In search for novel drug targets aimed to control CF lung infections, a key role of the non-lysosomal glucosidase 2 (GBA2-encoded GNLase) in proinflammatory state characterizing CF cells has been highlighted. As matter of fact, Miglustat® (d-NBDNJ) has been found to reduce the inflammatory response in P. aeruginosa infected CF bronchial cells showing a therapeutic potential of iminosugars in CF lung disease treatment. However, pharmacological use of d-iminosugars is hampered by their poor in vivo selectivity. Conversely, their non-superimposable mirror image, L-iminosugars have shown higher selectivity acting as inhibitors or enhancers of glycosidases and glycosyltransferasesI documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.


