Ontology highlight
ABSTRACT:
SUBMITTER: Yefidoff-Freedman R
PROVIDER: S-EPMC5567831 | biostudies-literature | 2017 Jul
REPOSITORIES: biostudies-literature
Yefidoff-Freedman Revital R Fan Jing J Yan Lu L Zhang Qingwen Q Dos Santos Guillermo Rodrigo Reis GRR Rana Sandeep S Contreras Jacob I JI Sahoo Rupam R Wan Debin D Young Jun J Dias Teixeira Karina Luiza KL Morisseau Christophe C Halperin Jose J Hammock Bruce B Natarajan Amarnath A Wang Peimin P Chorev Michael M Aktas Bertal H BH
Journal of medicinal chemistry 20170619 13
Heme-regulated inhibitor (HRI), an eukaryotic translation initiation factor 2 alpha (eIF2α) kinase, plays critical roles in cell proliferation, differentiation, adaptation to stress, and hemoglobin disorders. HRI phosphorylates eIF2α, which couples cellular signals, including endoplasmic reticulum (ER) stress, to translation. We previously identified 1,3-diarylureas and 1-((1,4-trans)-4-aryloxycyclohexyl)-3-arylureas (cHAUs) as specific activators of HRI that trigger the eIF2α phosphorylation ar ...[more]