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  4. Molecular Basis for Differential Patterns of Drug Resistance in Influenza N1 and N2 Neuraminidase
 
research article

Molecular Basis for Differential Patterns of Drug Resistance in Influenza N1 and N2 Neuraminidase

Prachanronarong, Kristina L.
•
Ozen, Aysegul
•
Thayer, Kelly M.
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2016
Journal of Chemical Theory and Computation

Neuraminidase (NA) inhibitors are used for the prevention and treatment of influenza A virus infections. Two subtypes of NA, N1 and N2, predominate in viruses that infect humans, but differential patterns of drug resistance have emerged in each subtype despite highly homologous active sites. To understand the molecular basis for the selection of these drug resistance mutations, structural and dynamic analyses on complexes of N1 and N2 NA with substrates and inhibitors were performed. Comparison of dynamic substrate and inhibitor envelopes and interactions at the active site revealed how differential patterns of drug resistance have emerged for specific drug resistance mutations, at residues I222, S246, and H274 in N1 and E119 in N2. Our results show that the differences in intermolecular interactions, especially van der Waals contacts, of the inhibitors versus substrates at the NA active site effectively explain the selection of resistance mutations in the two subtypes. Avoiding such contacts that render inhibitors vulnerable to resistance by better mimicking the dynamics and intermolecular interactions of substrates can lead to the development of novel inhibitors that avoid drug resistance in both subtypes.

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Type
research article
DOI
10.1021/acs.jctc.6b00703
Web of Science ID

WOS:000389866500035

Author(s)
Prachanronarong, Kristina L.
Ozen, Aysegul
Thayer, Kelly M.
Yilmaz, L. Safak
Zeldovich, Konstantin B.
Bolon, Daniel N.
Kowalik, Timothy F.
Jensen, Jeffrey D.  
Finberg, Robert W.
Wang, Jennifer P.
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Date Issued

2016

Publisher

Amer Chemical Soc

Published in
Journal of Chemical Theory and Computation
Volume

12

Issue

12

Start page

6098

End page

6108

Editorial or Peer reviewed

REVIEWED

Written at

EPFL

EPFL units
UPJENSEN  
Available on Infoscience
January 24, 2017
Use this identifier to reference this record
https://infoscience.epfl.ch/handle/20.500.14299/133567
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