IPA, a potent second-generation IRE1 activator of low molecular weight, activates the RNase domain via interaction with ATP-binding site, which in turn predisposes the kinase domain to …

2015年5月19日 · We engineered a potent small molecule, IPA, that binds to IRE1's ATP-binding pocket and predisposes the kinase domain to oligomerization, activating its RNase. IPA also …

2020年12月14日 · The RNase activity of Inositol-Requiring Enzyme 1 (IRE1) can be allosterically regulated by ATP-competitive inhibitors of the IRE1 kinase domain.

2024年5月7日 · Here we report that, in mammalian cells, formation of IRE1α clusters is an ER membrane-bound phase separation event that is coupled to the assembly of stress granules …

potent small molecule, IPA, that binds to IRE1’s ATP-binding pocket and predisposes the kinase domain to oligomerization, activating its RNase. IPA also inhibits PERK but, paradoxically, …

2015年5月19日 · We engineered a potent small molecule, IPA, that binds to IRE1's ATP-binding pocket and predisposes the kinase domain to oligomerization, activating its RNase. IPA also …

2024年4月1日 · IRE1 is an ER-resident type 1 transmembrane protein that comprises both BiP-binding (binding-immunoglobulin protein) and misfolded protein binding domain in the ER …

2024年6月1日 · NF-κB and XBP1 signaling was in turn activated by the endoplasmic reticulum (ER)-stress sensor inositol-requiring enzyme 1 (IRE1), which mediates the unfolded protein …

In the endoplasmic reticulum, unfolded proteins stimulate Ire1 autophosphorylation and RNase activity. The crystal structure of the dephosphorylated kinase/RNase domain of human Ire1 …

2021年2月5日 · Inositol-requiring enzyme type 1 (IRE1) is a serine/threonine kinase acting as one of three branches of the Unfolded Protein Response (UPR) signaling pathway, which is …