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Size and Flexibility Define the Inhibition of the H3N2 Influenza Endonuclease Enzyme by Calix[n]arenes

Authors :
Anthony W. Coleman
José P. Cerón-Carrasco
Horacio Pérez-Sánchez
Yannick Tauran
Moez Rhimi
Dominique Collard
Beom Joon Kim
Florent Perret
Laboratory for Integrated Micro Mechatronics Systems (LIMMS)
The University of Tokyo (UTokyo)-Centre National de la Recherche Scientifique (CNRS)
Laboratoire des Multimatériaux et Interfaces (LMI)
Université Claude Bernard Lyon 1 (UCBL)
Université de Lyon-Université de Lyon-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
UCAM
MICrobiologie de l'ALImentation au Service de la Santé (MICALIS)
Institut National de la Recherche Agronomique (INRA)-AgroParisTech
Institut de Chimie et Biochimie Moléculaires et Supramoléculaires (ICBMS)
Université de Lyon-Université de Lyon-Institut National des Sciences Appliquées de Lyon (INSA Lyon)
Université de Lyon-Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-Institut de Chimie du CNRS (INC)-École Supérieure Chimie Physique Électronique de Lyon-Centre National de la Recherche Scientifique (CNRS)
The University of Tokyo (UTokyo)
Institut Supérieur de l'Electronique et du Numérique - Lille (ISEN-Lille)
Institut supérieur de l'électronique et du numérique (ISEN)
AgroParisTech-Université Paris-Saclay-Institut National de Recherche pour l’Agriculture, l’Alimentation et l’Environnement (INRAE)
The University of Tokyo-Centre National de la Recherche Scientifique (CNRS)
Université de Lyon-Université de Lyon-Centre National de la Recherche Scientifique (CNRS)
Université de Lyon-Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-École Supérieure Chimie Physique Électronique de Lyon-Centre National de la Recherche Scientifique (CNRS)
The University of Tokyo
Source :
Antibiotics, Antibiotics, MDPI, 2019, 8 (2), pp.73. ⟨10.3390/antibiotics8020073⟩, Volume 8, Issue 2, Antibiotics 2 (8), 1-15. (2019), Antibiotics, Vol 8, Iss 2, p 73 (2019), Antibiotics and Chemotherapy-Basel, Antibiotics and Chemotherapy-Basel-, 2019, 8 (2), pp.73. ⟨10.3390/antibiotics8020073⟩
Publication Year :
2019
Publisher :
MDPI AG, 2019.

Abstract

Inhibition of H3N2 influenza PA endonuclease activity by a panel of anionic calix[n]arenes and &beta<br />cyclodextrin sulfate has been studied. The joint experimental and theoretical results reveal that the larger, more flexible and highly water-soluble sulfonato-calix[n]arenes have high inhibitory activity, with para-sulfonato-calix[8]arene, SC8, having an IC50 value of 6.4 &mu<br />M. Molecular docking calculations show the SC8 can interact at both the polyanion binding site and also the catalytic site of H3N2 influenza PA endonuclease.

Subjects

Subjects :
0301 basic medicine
Microbiology (medical)
h3n2 virus
Stereochemistry
viruses
enzyme inhibitors
[SDV]Life Sciences [q-bio]
anti-viral activity
calix[n]arene
complex mixtures
01 natural sciences
Biochemistry
Microbiology
Article
endonuclease
Catalysis
03 medical and health sciences
Endonuclease
molecular docking
[SDV.BBM]Life Sciences [q-bio]/Biochemistry, Molecular Biology
Pharmacology (medical)
General Pharmacology, Toxicology and Pharmaceutics
Binding site
IC50
ComputingMilieux_MISCELLANEOUS
chemistry.chemical_classification
biology
010405 organic chemistry
Chemistry
lcsh:RM1-950
virus diseases
[CHIM.MATE]Chemical Sciences/Material chemistry
respiratory tract diseases
0104 chemical sciences
3. Good health
lcsh:Therapeutics. Pharmacology
[SDV.MP]Life Sciences [q-bio]/Microbiology and Parasitology
030104 developmental biology
Infectious Diseases
Enzyme
biology.protein

Details

ISSN :
20796382 and 00664758
Volume :
8
Database :
OpenAIRE
Journal :
Antibiotics
Accession number :
edsair.doi.dedup.....b715e353eb2ef0499f4a0218e6100a43
Full Text :
https://doi.org/10.3390/antibiotics8020073
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