Structure Elucidation of Coxsackievirus A16 in Complex with GPP3 Informs a Systematic Review of Highly Potent Capsid Binders to Enteroviruses.

The replication of enterovirus 71 (EV71) and coxsackievirus A16 (CVA16), which are the major cause of hand, foot and mouth disease (HFMD) in children, can be inhibited by the capsid binder GPP3. Here, we present the crystal structure of CVA16 in complex with GPP3, which clarifies the role of the key...

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Main Authors: Luigi De Colibus, Xiangxi Wang, Aloys Tijsma, Johan Neyts, John A B Spyrou, Jingshan Ren, Jonathan M Grimes, Gerhard Puerstinger, Pieter Leyssen, Elizabeth E Fry, Zihe Rao, David I Stuart
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2015-10-01
Series:PLoS Pathogens
Online Access:https://doi.org/10.1371/journal.ppat.1005165
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author Luigi De Colibus
Xiangxi Wang
Aloys Tijsma
Johan Neyts
John A B Spyrou
Jingshan Ren
Jonathan M Grimes
Gerhard Puerstinger
Pieter Leyssen
Elizabeth E Fry
Zihe Rao
David I Stuart
author_facet Luigi De Colibus
Xiangxi Wang
Aloys Tijsma
Johan Neyts
John A B Spyrou
Jingshan Ren
Jonathan M Grimes
Gerhard Puerstinger
Pieter Leyssen
Elizabeth E Fry
Zihe Rao
David I Stuart
author_sort Luigi De Colibus
collection DOAJ
description The replication of enterovirus 71 (EV71) and coxsackievirus A16 (CVA16), which are the major cause of hand, foot and mouth disease (HFMD) in children, can be inhibited by the capsid binder GPP3. Here, we present the crystal structure of CVA16 in complex with GPP3, which clarifies the role of the key residues involved in interactions with the inhibitor. Based on this model, in silico docking was performed to investigate the interactions with the two next-generation capsid binders NLD and ALD, which we show to be potent inhibitors of a panel of enteroviruses with potentially interesting pharmacological properties. A meta-analysis was performed using the available structural information to obtain a deeper insight into those structural features required for capsid binders to interact effectively and also those that confer broad-spectrum anti-enterovirus activity.
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publisher Public Library of Science (PLoS)
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series PLoS Pathogens
spelling doaj-art-d89b91dd3ef940ec81e2edbd8ac8c24a2025-08-20T03:10:05ZengPublic Library of Science (PLoS)PLoS Pathogens1553-73661553-73742015-10-011110e100516510.1371/journal.ppat.1005165Structure Elucidation of Coxsackievirus A16 in Complex with GPP3 Informs a Systematic Review of Highly Potent Capsid Binders to Enteroviruses.Luigi De ColibusXiangxi WangAloys TijsmaJohan NeytsJohn A B SpyrouJingshan RenJonathan M GrimesGerhard PuerstingerPieter LeyssenElizabeth E FryZihe RaoDavid I StuartThe replication of enterovirus 71 (EV71) and coxsackievirus A16 (CVA16), which are the major cause of hand, foot and mouth disease (HFMD) in children, can be inhibited by the capsid binder GPP3. Here, we present the crystal structure of CVA16 in complex with GPP3, which clarifies the role of the key residues involved in interactions with the inhibitor. Based on this model, in silico docking was performed to investigate the interactions with the two next-generation capsid binders NLD and ALD, which we show to be potent inhibitors of a panel of enteroviruses with potentially interesting pharmacological properties. A meta-analysis was performed using the available structural information to obtain a deeper insight into those structural features required for capsid binders to interact effectively and also those that confer broad-spectrum anti-enterovirus activity.https://doi.org/10.1371/journal.ppat.1005165
spellingShingle Luigi De Colibus
Xiangxi Wang
Aloys Tijsma
Johan Neyts
John A B Spyrou
Jingshan Ren
Jonathan M Grimes
Gerhard Puerstinger
Pieter Leyssen
Elizabeth E Fry
Zihe Rao
David I Stuart
Structure Elucidation of Coxsackievirus A16 in Complex with GPP3 Informs a Systematic Review of Highly Potent Capsid Binders to Enteroviruses.
PLoS Pathogens
title Structure Elucidation of Coxsackievirus A16 in Complex with GPP3 Informs a Systematic Review of Highly Potent Capsid Binders to Enteroviruses.
title_full Structure Elucidation of Coxsackievirus A16 in Complex with GPP3 Informs a Systematic Review of Highly Potent Capsid Binders to Enteroviruses.
title_fullStr Structure Elucidation of Coxsackievirus A16 in Complex with GPP3 Informs a Systematic Review of Highly Potent Capsid Binders to Enteroviruses.
title_full_unstemmed Structure Elucidation of Coxsackievirus A16 in Complex with GPP3 Informs a Systematic Review of Highly Potent Capsid Binders to Enteroviruses.
title_short Structure Elucidation of Coxsackievirus A16 in Complex with GPP3 Informs a Systematic Review of Highly Potent Capsid Binders to Enteroviruses.
title_sort structure elucidation of coxsackievirus a16 in complex with gpp3 informs a systematic review of highly potent capsid binders to enteroviruses
url https://doi.org/10.1371/journal.ppat.1005165
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