TY - JOUR
T1 - The capsid binder vapendavir and the novel protease inhibitor SG85 inhibit enterovirus 71 replication
AU - Tijsma, Aloys
AU - Franco, David
AU - Tucker, Simon
AU - Hilgenfeld, Rolf
AU - Froeyen, Mathy
AU - Leyssen, Pieter
AU - Neyts, Johan
PY - 2014/11/1
Y1 - 2014/11/1
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=84908628085&partnerID=8YFLogxK
U2 - 10.1128/AAC.03328-14
DO - 10.1128/AAC.03328-14
M3 - Journal articles
C2 - 25199773
AN - SCOPUS:84908628085
SN - 0066-4804
VL - 58
SP - 6990
EP - 6992
JO - Antimicrobial Agents and Chemotherapy
JF - Antimicrobial Agents and Chemotherapy
IS - 11
ER -