Article
Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors.
Nature chemical biology - 1 Dec 2012
Wang Likun, Perera B Gayani K, Hari Sanjay B, Bhhatarai Barun, Backes Bradley J, Seeliger Markus A, Schürer Stephan C, Oakes Scott A, Papa Feroz R, Maly Dustin J
Abstract excerpt
Under endoplasmic reticulum stress, unfolded protein accumulation leads to activation of the endoplasmic reticulum transmembrane kinase/endoRNase (RNase) IRE1α. IRE1α oligomerizes, autophosphorylates and initiates splicing of XBP1 mRNA, thus triggering the unfolded protein response (UPR). Here we show that IRE1α's kinase-controlled RNase can be regulated in two distinct modes with kinase inhibitors: one class of...
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