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Delivery of Suramin as an Antiviral Agent through Liposomal Systems

Academic Article
Publication Date:
2014
abstract:
Norovirus RNA-dependent RNA polymerase (RdRp) is a promising target enzyme for the development of new antiviral drugs. Starting from the crystal structure of norovirus RdRp, we had previously performed an in silico docking search using a library of low-molecular-weight compounds that enabled us to select molecules with predicted enzyme inhibitory activity. Among these, the polysulfonated naphthylurea suramin proved to inhibit in vitro both murine and human norovirus polymerases, with IC50 values in the low micromolar range. The negatively charged inhibitor, however, displayed poor cell permeability in cell-based experiments. Therefore, we produced different suramin-loaded liposome formulations and evaluated their activities in cell-based assays using murine norovirus cultivated in RAW 264.7 macrophages, as a model for norovirus genus. The results obtained show that suramin, when delivered through liposomes, can effectively inhibit murine norovirus replication.
Iris type:
01.01 Articolo in rivista
Keywords:
antiviral agents; drug delivery; liposomes; norovirus; RNA-dependent RNA polymerase
List of contributors:
Bolognesi, Martino; Pezzullo, Margherita; MILANI DE MAYO DE MARI, Mario; Mastrangelo, Eloise
Authors of the University:
MASTRANGELO ELOISE
MILANI DE MAYO DE MARI MARIO
Handle:
https://iris.cnr.it/handle/20.500.14243/222821
Published in:
CHEMMEDCHEM (PRINT)
Journal
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