Title: The capsid binder vapendavir and the novel protease inhibitor SG85 inhibit enterovirus 71 replication
Authors: Tijsma, Aloys ×
Franco, David
Tucker, Simon
Hilgenfeld, Rolf
Froeyen, Mathy
Leyssen, Pieter
Neyts, Johan #
Issue Date: Nov-2014
Series Title: Antimicrobial agents and chemotherapy vol:58 issue:11 pages:6990-2
Article number: 10.1128/AAC.03328-14
Abstract: Antivirals against enterovirus 71 (EV71) are urgently needed. We demonstrate that the novel enteroviral protease inhibitor (PI) SG85 and capsid binder (CB) vapendavir efficiently inhibit the in vitro replication of 21 EV71 strains/isolates that are representative of the different genogroups A, B, and C. The PI rupintrivir, the CB pirodavir, and the host-targeting compound enviroxime, which were included as reference compounds, also inhibited the replication of all isolates. Remarkably, the CB compound pleconaril was devoid of any anti-EV71 activity. An in silico docking study revealed that pleconaril-unlike vapendavir and pirodavir-lacks essential binding interactions with the viral capsid. Vapendavir and SG85 (or analogues) should be further explored for the treatment of EV71 infections. The data presented here may serve as a reference when developing yet-novel inhibitors.
ISSN: 1098-6596
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
Medicinal Chemistry (Rega Institute)
× corresponding author
# (joint) last author

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