Activation of the IRE1 RNase through remodeling of the kinase front pocket by ATP-competitive ligands
The RNase activity of Inositol-Requiring Enzyme 1 (IRE1) can be allosterically regulated by ATP-competitive inhibitors of the IRE1 kinase domain. Here, the authors identify ATP-competitive IRE1 RNase activators with improved selectivity and cellular activity, and elucidate their mechanism of action.
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Nature Portfolio
2020
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| Acceso en línea: | https://doaj.org/article/b949b998bea04b119070c87d6eced201 |
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oai:doaj.org-article:b949b998bea04b119070c87d6eced2012021-12-02T13:24:34ZActivation of the IRE1 RNase through remodeling of the kinase front pocket by ATP-competitive ligands10.1038/s41467-020-19974-52041-1723https://doaj.org/article/b949b998bea04b119070c87d6eced2012020-12-01T00:00:00Zhttps://doi.org/10.1038/s41467-020-19974-5https://doaj.org/toc/2041-1723The RNase activity of Inositol-Requiring Enzyme 1 (IRE1) can be allosterically regulated by ATP-competitive inhibitors of the IRE1 kinase domain. Here, the authors identify ATP-competitive IRE1 RNase activators with improved selectivity and cellular activity, and elucidate their mechanism of action.Elena FerriAdrien Le ThomasHeidi Ackerly WallweberEric S. DayBenjamin T. WaltersSusan E. KaufmanMarie-Gabrielle BraunKevin R. ClarkMaureen H. BeresiniKyle MortaraYung-Chia A. ChenBreanna CanterWilson PhungPeter S. LiuAlfred LammensAvi AshkenaziJoachim RudolphWeiru WangNature PortfolioarticleScienceQENNature Communications, Vol 11, Iss 1, Pp 1-15 (2020) |
| institution |
DOAJ |
| collection |
DOAJ |
| language |
EN |
| topic |
Science Q |
| spellingShingle |
Science Q Elena Ferri Adrien Le Thomas Heidi Ackerly Wallweber Eric S. Day Benjamin T. Walters Susan E. Kaufman Marie-Gabrielle Braun Kevin R. Clark Maureen H. Beresini Kyle Mortara Yung-Chia A. Chen Breanna Canter Wilson Phung Peter S. Liu Alfred Lammens Avi Ashkenazi Joachim Rudolph Weiru Wang Activation of the IRE1 RNase through remodeling of the kinase front pocket by ATP-competitive ligands |
| description |
The RNase activity of Inositol-Requiring Enzyme 1 (IRE1) can be allosterically regulated by ATP-competitive inhibitors of the IRE1 kinase domain. Here, the authors identify ATP-competitive IRE1 RNase activators with improved selectivity and cellular activity, and elucidate their mechanism of action. |
| format |
article |
| author |
Elena Ferri Adrien Le Thomas Heidi Ackerly Wallweber Eric S. Day Benjamin T. Walters Susan E. Kaufman Marie-Gabrielle Braun Kevin R. Clark Maureen H. Beresini Kyle Mortara Yung-Chia A. Chen Breanna Canter Wilson Phung Peter S. Liu Alfred Lammens Avi Ashkenazi Joachim Rudolph Weiru Wang |
| author_facet |
Elena Ferri Adrien Le Thomas Heidi Ackerly Wallweber Eric S. Day Benjamin T. Walters Susan E. Kaufman Marie-Gabrielle Braun Kevin R. Clark Maureen H. Beresini Kyle Mortara Yung-Chia A. Chen Breanna Canter Wilson Phung Peter S. Liu Alfred Lammens Avi Ashkenazi Joachim Rudolph Weiru Wang |
| author_sort |
Elena Ferri |
| title |
Activation of the IRE1 RNase through remodeling of the kinase front pocket by ATP-competitive ligands |
| title_short |
Activation of the IRE1 RNase through remodeling of the kinase front pocket by ATP-competitive ligands |
| title_full |
Activation of the IRE1 RNase through remodeling of the kinase front pocket by ATP-competitive ligands |
| title_fullStr |
Activation of the IRE1 RNase through remodeling of the kinase front pocket by ATP-competitive ligands |
| title_full_unstemmed |
Activation of the IRE1 RNase through remodeling of the kinase front pocket by ATP-competitive ligands |
| title_sort |
activation of the ire1 rnase through remodeling of the kinase front pocket by atp-competitive ligands |
| publisher |
Nature Portfolio |
| publishDate |
2020 |
| url |
https://doaj.org/article/b949b998bea04b119070c87d6eced201 |
| work_keys_str_mv |
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| _version_ |
1718393054812962816 |