Orally Active Fusion Inhibitor of Respiratory Syncytial Virus
AUTOR(ES)
Cianci, Christopher
FONTE
American Society for Microbiology
RESUMO
BMS-433771 was found to be a potent inhibitor of respiratory syncytial virus (RSV) replication in vitro. It exhibited excellent potency against multiple laboratory and clinical isolates of both group A and B viruses, with an average 50% effective concentration of 20 nM. Mechanism-of-action studies demonstrated that BMS-433771 inhibits the fusion of lipid membranes during both the early virus entry stage and late-stage syncytium formation. After isolation of resistant viruses, resistance was mapped to a series of single amino acid mutations in the F1 subunit of the fusion protein. Upon oral administration, BMS-433771 was able to reduce viral titers in the lungs of mice infected with RSV. This new class of orally active RSV fusion inhibitors offers potential for clinical development.
ACESSO AO ARTIGO
http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=321540Documentos Relacionados
- Antigenic Structure of Human Respiratory Syncytial Virus Fusion Glycoprotein
- RFI-641, a Potent Respiratory Syncytial Virus Inhibitor
- Structural characterization of the human respiratory syncytial virus fusion protein core
- Monoclonal antibodies to the fusion protein of bovine respiratory syncytial virus.
- Monoclonal antibodies to respiratory syncytial virus proteins: identification of the fusion protein.
