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Antimicrob Agents Chemother. 2015 Sep;59(9):5814-8. doi: 10.1128/AAC.00534-15. Epub 2015 Jun 8.

The enterovirus 3C protease inhibitor SG85 efficiently blocks rhinovirus replication and is not cross-resistant with rupintrivir.

Author information

1
Laboratory for Virology, Rega Institute for Medical Research, KU Leuven, Leuven, Belgium.
2
Institute of Biochemistry, Center for Structural and Cell Biology in Medicine, University of Lübeck, Lübeck, Germany.
3
Institute of Biochemistry, Center for Structural and Cell Biology in Medicine, University of Lübeck, Lübeck, Germany German Center for Infection Research (DZIF), Hamburg-Lübeck-Borstel Site, University of Lübeck, Lübeck, Germany.
4
Laboratory for Virology, Rega Institute for Medical Research, KU Leuven, Leuven, Belgium johan.neyts@rega.kuleuven.be.

Abstract

The novel enterovirus protease inhibitor (PI) SG85 effectively inhibits the in vitro replication of 14 rhinoviruses representative of species A and B (median 50% effective concentration, 0.04 μM). A low-level SG85-resistant variant was selected that carried amino acid substitutions S127G and T143A in the 3C protease. Both substitutions are required for low-level resistance to SG85, as demonstrated by reverse genetics. Interestingly, there is no cross-resistance to SG85 and rupintrivir (another PI); a structural explanation is provided for this observation.

PMID:
26055377
PMCID:
PMC4538484
DOI:
10.1128/AAC.00534-15
[Indexed for MEDLINE]
Free PMC Article

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