[HTML][HTML] Potent and selective inhibitors of the inositol-requiring enzyme 1 endoribonuclease
K Volkmann, JL Lucas, D Vuga, X Wang… - Journal of Biological …, 2011 - ASBMB
Inositol-requiring enzyme 1 (IRE1) is the most highly conserved signaling node of the
unfolded protein response (UPR) and represents a potential therapeutic target for a number
of diseases associated with endoplasmic reticulum stress. IRE1 activates the XBP-1
transcription factor by site-specific cleavage of two hairpin loops within its mRNA to facilitate
its nonconventional splicing and alternative translation. We screened for inhibitors using a
construct containing the unique cytosolic kinase and endoribonuclease domains of human …
unfolded protein response (UPR) and represents a potential therapeutic target for a number
of diseases associated with endoplasmic reticulum stress. IRE1 activates the XBP-1
transcription factor by site-specific cleavage of two hairpin loops within its mRNA to facilitate
its nonconventional splicing and alternative translation. We screened for inhibitors using a
construct containing the unique cytosolic kinase and endoribonuclease domains of human …