Figure 4: SAR of HAA inhibitors and their binding site on IRE1α. | Nature Communications

Figure 4: SAR of HAA inhibitors and their binding site on IRE1α.

From: Structure and mechanism of action of the hydroxy–aryl–aldehyde class of IRE1 endoribonuclease inhibitors

Figure 4

(a) Schematic (left) and SDS–PAGE analysis (right) of IRE1α RNase-active site mutants. (b) Effect of RNase-active site mutations on IRE1α RNase function as assessed by a real-time fluorescence readout assay. (c) Effect of RNase-active site mutations on IRE1α kinase function as assessed by auto-kinase activity (phosphor image, top; quantification, bottom). (d) Sensitivity of IRE1α wild-type (WT) and RNase-active site mutants to inhibition of RNase activity by MKC9989 as assessed using a dual-hairpin RNA substrate.

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