Hearn, Brian R. published the artcileStructure-Activity Studies of Bis-O-Arylglycolamides: Inhibitors of the Integrated Stress Response, Application of 2-(4-(Trifluoromethyl)phenoxy)acetic acid, the publication is ChemMedChem (2016), 11(8), 870-880, database is CAplus and MEDLINE.
The integrated stress response (ISR) comprises multiple signaling pathways for detecting and responding to cellular stress that converge at a single event – the phosphorylation of Ser51 on the ¦Á-subunit of eukaryotic translation initiation factor 2 (eIF2¦Á). Phosphorylation of eIF2¦Á (eIF2¦Á-P) results in attenuation of global protein synthesis via the inhibitory effects of eIF2¦Á-P on eIF2B, the guanine exchange factor (GEF) for eIF2. Herein we describe structure-activity relationship (SAR) studies of bis-O-arylglycolamides, first-in-class integrated stress response inhibitors (ISRIB). ISRIB analogs make cells insensitive to the effects of eIF2¦Á-P by activating the GEF activity of eIF2B and allowing global protein synthesis to proceed with residual unphosphorylated eIF2¦Á. The SAR studies described herein support the proposed pharmacol. of ISRIB analogs as binding across a sym. protein-protein interface formed between protein subunits of the dimeric eIF2B heteropentamer.
ChemMedChem published new progress about 163839-73-4. 163839-73-4 belongs to catalysis-chemistry, auxiliary class Trifluoromethyl,Fluoride,Carboxylic acid,Benzene,Ether, name is 2-(4-(Trifluoromethyl)phenoxy)acetic acid, and the molecular formula is C9H7F3O3, Application of 2-(4-(Trifluoromethyl)phenoxy)acetic acid.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia