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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Feldman, H.C., Maly, D.J. (2017). Profiling the Dual Enzymatic Activities of the Serine/Threonine Kinase IRE1α. In: Kasid, U., Clarke, R. (eds) Cancer Gene Networks. Methods in Molecular Biology, vol 1513. Humana Press, New York, NY. https://doi.org/10.1007/978-1-4939-6539-7_17
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DOI: https://doi.org/10.1007/978-1-4939-6539-7_17
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Publisher Name: Humana Press, New York, NY
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