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pH-sensitive liposomes are efficient carriers for endoplasmic reticulum targeted drugs in mouse melanoma cells

Domenii publicaţii > Biologie + Tipuri publicaţii > Articol în revistã ştiinţificã

Autori: Costin, G.-E., Trif, M., Nichita, N., Dwek, R. A., Petrescu, S. M.

Editorial: BBRC, 293 (3), p.918-923, 2002.


Tyrosinase, the key enzyme of melanin biosynthesis, is inactivated in melanoma cells following the incubation with the imino-sugar N-butyldeoxynojirimycin, an inhibitor of the endoplasmic reticulum N-glycosylation processing. We have previously shown that tyrosinase inhibition requires high NB-DNJ concentrations, suggesting an inefficient cellular uptake of the drug. Here we show that the use of pH-sensitive liposomes composed of dioleoylphosphatidylethanolamine and cholesteryl hemisuccinate for the delivery of NB-DNJ reduced the required dose for tyrosinase inhibition by a factor of 1000. The results indicate that these pH-sensitive liposomes are efficient carriers for imino-sugars delivery in the endoplasmic reticulum of mammalian cells. (c) 2002 Elsevier Science (USA).

Cuvinte cheie: journal