Please use this identifier to cite or link to this item: https://doi.org/10.1038/srep33663
Title: Antiviral activities of peptide-based covalent inhibitors of the Enterovirus 71 3C protease
Authors: Tan, Yong Wah
Ang, Melgious Jin Yan
Lau, Qiu Ying
Poulsen, Anders
NG FUI MEE 
Then, Siew Wen
Peng, Jianhe
HILL, JEFFREY 
Hong Wan Jin 
Chia, Cheng San Brian
CHU JANG HANN 
Keywords: Antiviral Agents
Cell Line
Cysteine Endopeptidases
Drug Evaluation, Preclinical
Drug Synergism
Enterovirus
Enterovirus A, Human
Humans
Inhibitory Concentration 50
Peptides
Protease Inhibitors
Viral Proteins
Virus Replication
Issue Date: 20-Sep-2016
Publisher: Springer Science and Business Media LLC
Citation: Tan, Yong Wah, Ang, Melgious Jin Yan, Lau, Qiu Ying, Poulsen, Anders, NG FUI MEE, Then, Siew Wen, Peng, Jianhe, HILL, JEFFREY, Hong Wan Jin, Chia, Cheng San Brian, CHU JANG HANN (2016-09-20). Antiviral activities of peptide-based covalent inhibitors of the Enterovirus 71 3C protease. SCIENTIFIC REPORTS 6 (1) : 33663-. ScholarBank@NUS Repository. https://doi.org/10.1038/srep33663
Abstract: © 2016 The Author(s). Hand, Foot and Mouth Disease is a highly contagious disease caused by a range of human enteroviruses. Outbreaks occur regularly, especially in the Asia-Pacific region, putting a burden on public healthcare systems. Currently, there is no antiviral for treating this infectious disease and the only vaccines are limited to circulation in China, presenting an unmet medical need that needs to be filled urgently. The human enterovirus 3 C protease has been deemed a plausible drug target due to its essential roles in viral replication. In this study, we designed and synthesized 10 analogues of the Rhinovirus 3 C protease inhibitor, Rupintrivir, and tested their 3 C protease inhibitory activities followed by a cellular assay using human enterovirus 71 (EV71)-infected human RD cells. Our results revealed that a peptide-based compound containing a trifluoromethyl moiety to be the most potent analogue, with an EC 50 of 65 nM, suggesting its potential as a lead for antiviral drug discovery.
Source Title: SCIENTIFIC REPORTS
URI: https://scholarbank.nus.edu.sg/handle/10635/170678
ISSN: 2045-2322
DOI: 10.1038/srep33663
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