Peptidomimetic‐based identification of FDA‐approved compounds inhibiting IRE1 activity

• Published in: The FEBS journal Vol. 288; no. 3; pp. 945 - 960
• Main Authors: Doultsinos, Dimitrios, Carlesso, Antonio, Chintha, Chetan, Paton, James C., Paton, Adrienne W., Samali, Afshin, Chevet, Eric, Eriksson, Leif A.
• Format: Journal Article
• Language: English
• Published: England Blackwell Publishing Ltd 01.02.2021; Wiley
• Subjects: Biochemistry & Molecular Biology; Biochemistry and Molecular Biology; Biokemi och molekylärbiologi; Cancer; Cefoperazone; Cell culture; Chemotherapy; docking; Endoplasmic reticulum; Fludarabine; Folinic acid; glide; Glioblastoma; Glioblastoma cells; Human performance; Hypoxia; Inhibitors; Inositol; IRE1; ire1-alpha; Kinases; Life Sciences; Methotrexate; Optimization; peptides; Protein folding; Protein-serine/threonine kinase; Proteins; response; selective-inhibition; Temozolomide; Tumors; unfolded protein; unfolded protein response; inhibitors; unfolded protein response; glioblastoma; endoplasmic reticulum; IRE1; Inhibitors; Endoplasmic Reticulum; Unfolded Protein Response

Inositol‐requiring enzyme 1 (IRE1) is a bifunctional serine/threonine kinase and endoribonuclease that is a major mediator of the unfolded protein response (UPR) during endoplasmic reticulum (ER) stress. Tumour cells experience ER stress due to adverse environmental cues such as hypoxia or nutrient...