ArticleACS bio & med chem Au2026
Pyrazolylpyrimidinamines Decorated via Petasis Reaction as Small-Molecule Activators of the RNA-Degrading Ribonuclease IRE1α.
Article in ACS bio & med chem Au, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
The multicomponent Petasis boron-Mannich reaction (PR) enables the generation of functionalized amines that are of biological interest. Here, we demonstrated that a series of pyrazolylpyrimidinamines decorated via PR are new small-molecule activators of the dual kinase and ribonuclease RNA-degrading protein inositol-requiring enzyme 1α (IRE1α), which is an essential effector in the unfolded protein response associated with many human diseases. Compound SH4 was identified via a FRET assay and showed potent activity in activating the IRE1α ribonuclease (RNase) activity, inducing increased
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