Binding of ISRIB reveals a regulatory site in the nucleotide exchange factor eIF2B

The integrated stress response (ISR) is a conserved translational and transcriptional program affecting metabolism, memory, and immunity. The ISR is mediated by stress-induced phosphorylation of eukaryotic translation initiation factor 2α (eIF2α) that attenuates the guanine nucleotide exchange facto...

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Main Authors: Zyryanova, Alisa F., Weis, Félix, Faille, Alexandre, Abo Alard, Akeel, Crespillo-Casado, Ana, Sekine, Yusuke, Harding, Heather P., Allen, Felicity, Parts, Leopold, Fromont, Christoph, Fischer, Peter M., Warren, Alan J., Ron, David
Format: Article
Language:English
Published: American Association for the Advancement of Science 2018
Online Access:https://eprints.nottingham.ac.uk/50909/
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author Zyryanova, Alisa F.
Weis, Félix
Faille, Alexandre
Abo Alard, Akeel
Crespillo-Casado, Ana
Sekine, Yusuke
Harding, Heather P.
Allen, Felicity
Parts, Leopold
Fromont, Christoph
Fischer, Peter M.
Warren, Alan J.
Ron, David
author_facet Zyryanova, Alisa F.
Weis, Félix
Faille, Alexandre
Abo Alard, Akeel
Crespillo-Casado, Ana
Sekine, Yusuke
Harding, Heather P.
Allen, Felicity
Parts, Leopold
Fromont, Christoph
Fischer, Peter M.
Warren, Alan J.
Ron, David
author_sort Zyryanova, Alisa F.
building Nottingham Research Data Repository
collection Online Access
description The integrated stress response (ISR) is a conserved translational and transcriptional program affecting metabolism, memory, and immunity. The ISR is mediated by stress-induced phosphorylation of eukaryotic translation initiation factor 2α (eIF2α) that attenuates the guanine nucleotide exchange factor eIF2B. A chemical inhibitor of the ISR, ISRIB, reverses the attenuation of eIF2B by phosphorylated eIF2α, protecting mice from neurodegeneration and traumatic brain injury. We describe a 4.1-angstrom-resolution cryo–electron microscopy structure of human eIF2B with an ISRIB molecule bound at the interface between the β and δ regulatory subunits. Mutagenesis of residues lining this pocket altered the hierarchical cellular response to ISRIB analogs in vivo and ISRIB binding in vitro. Our findings point to a site in eIF2B that can be exploited by ISRIB to regulate translation.
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spelling nottingham-509092018-09-30T04:30:14Z https://eprints.nottingham.ac.uk/50909/ Binding of ISRIB reveals a regulatory site in the nucleotide exchange factor eIF2B Zyryanova, Alisa F. Weis, Félix Faille, Alexandre Abo Alard, Akeel Crespillo-Casado, Ana Sekine, Yusuke Harding, Heather P. Allen, Felicity Parts, Leopold Fromont, Christoph Fischer, Peter M. Warren, Alan J. Ron, David The integrated stress response (ISR) is a conserved translational and transcriptional program affecting metabolism, memory, and immunity. The ISR is mediated by stress-induced phosphorylation of eukaryotic translation initiation factor 2α (eIF2α) that attenuates the guanine nucleotide exchange factor eIF2B. A chemical inhibitor of the ISR, ISRIB, reverses the attenuation of eIF2B by phosphorylated eIF2α, protecting mice from neurodegeneration and traumatic brain injury. We describe a 4.1-angstrom-resolution cryo–electron microscopy structure of human eIF2B with an ISRIB molecule bound at the interface between the β and δ regulatory subunits. Mutagenesis of residues lining this pocket altered the hierarchical cellular response to ISRIB analogs in vivo and ISRIB binding in vitro. Our findings point to a site in eIF2B that can be exploited by ISRIB to regulate translation. American Association for the Advancement of Science 2018-03-30 Article PeerReviewed application/pdf en https://eprints.nottingham.ac.uk/50909/1/Zyryanova%2C%20A.F.%20et%20al.%20Science%202018%20author%20version.pdf Zyryanova, Alisa F., Weis, Félix, Faille, Alexandre, Abo Alard, Akeel, Crespillo-Casado, Ana, Sekine, Yusuke, Harding, Heather P., Allen, Felicity, Parts, Leopold, Fromont, Christoph, Fischer, Peter M., Warren, Alan J. and Ron, David (2018) Binding of ISRIB reveals a regulatory site in the nucleotide exchange factor eIF2B. Science, 359 (6383). pp. 1533-1536. ISSN 1095-9203 http://science.sciencemag.org/content/359/6383/1533.long doi:10.1126/science.aar5129 doi:10.1126/science.aar5129
spellingShingle Zyryanova, Alisa F.
Weis, Félix
Faille, Alexandre
Abo Alard, Akeel
Crespillo-Casado, Ana
Sekine, Yusuke
Harding, Heather P.
Allen, Felicity
Parts, Leopold
Fromont, Christoph
Fischer, Peter M.
Warren, Alan J.
Ron, David
Binding of ISRIB reveals a regulatory site in the nucleotide exchange factor eIF2B
title Binding of ISRIB reveals a regulatory site in the nucleotide exchange factor eIF2B
title_full Binding of ISRIB reveals a regulatory site in the nucleotide exchange factor eIF2B
title_fullStr Binding of ISRIB reveals a regulatory site in the nucleotide exchange factor eIF2B
title_full_unstemmed Binding of ISRIB reveals a regulatory site in the nucleotide exchange factor eIF2B
title_short Binding of ISRIB reveals a regulatory site in the nucleotide exchange factor eIF2B
title_sort binding of isrib reveals a regulatory site in the nucleotide exchange factor eif2b
url https://eprints.nottingham.ac.uk/50909/
https://eprints.nottingham.ac.uk/50909/
https://eprints.nottingham.ac.uk/50909/