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

AF Zyryanova, F Weis, A Faille, AA Alard… - Science, 2018 - science.org
AF Zyryanova, F Weis, A Faille, AA Alard, A Crespillo-Casado, Y Sekine, HP Harding…
Science, 2018science.org
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 …
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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