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  • Title: Profiling the Dual Enzymatic Activities of the Serine/Threonine Kinase IRE1α.
    Author: Feldman HC, Maly DJ.
    Journal: Methods Mol Biol; 2017; 1513():233-242. PubMed ID: 27807842.
    Abstract:
    There is an allosteric relationship between the kinase and RNase domains of the ER stress sensor IRE1α. This relationship has been exploited to develop ATP-competitive inhibitors that are able to divergently modulate the RNase activity of IRE1α through its kinase domain. Here, we describe a series of biochemical methods for profiling the dual enzymatic activities of IRE1α. These methods can be used to ascertain how ATP-competitive inhibitors affect the kinase activity of IRE1α and for determining whether these ligands allosterically activate or inactivate RNase activity.
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