| Title | The enterovirus 3C protease inhibitor SG85 efficiently blocks rhinovirus replication and is not cross-resistant with rupintrivir. | ||
| Author | Lacroix, Celine; George, Shyla; Leyssen, Pieter; Hilgenfeld, Rolf; Neyts, Johan | ||
| Journal | Antimicrob Agents Chemother | Publication Year/Month | 2015-Sep |
| PMID | 26055377 | PMCID | PMC4538484 |
| Affiliation + expend | 1.Laboratory for Virology, Rega Institute for Medical Research, KU Leuven, Leuven, Belgium. | ||
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 muM). 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.