The Enterovirus 3C Protease Inhibitor SG85 Efficiently Blocks Rhinovirus Replication and Is Not Cross-Resistant with Rupintrivir | Zendy

Céline Lacroix | Zendy; Shyla George | Zendy; Pieter Leyssen | Zendy; Rolf Hilgenfeld | Zendy; Johan Neyts | Zendy

Open Access

The Enterovirus 3C Protease Inhibitor SG85 Efficiently Blocks Rhinovirus Replication and Is Not Cross-Resistant with Rupintrivir

Author(s) -

Céline Lacroix,

Shyla George,

Pieter Leyssen,

Rolf Hilgenfeld,

Johan Neyts

Publication year - 2015

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.00534-15

Subject(s) - rhinovirus , protease , enterovirus , virology , protease inhibitor (pharmacology) , biology , in vitro , viral replication , replication (statistics) , enterovirus 71 , virus , chemistry , microbiology and biotechnology , enzyme , genetics , biochemistry , viral load , antiretroviral therapy

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.

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