In 2017,Yefidoff-Freedman, Revital; Fan, Jing; Yan, Lu; Zhang, Qingwen; dos Santos, Guillermo Rodrigo Reis; Rana, Sandeep; Contreras, Jacob I.; Sahoo, Rupam; Wan, Debin; Young, Jun; Dias Teixeira, Karina Luiza; Morisseau, Christophe; Halperin, Jose; Hammock, Bruce; Natarajan, Amarnath; Wang, Peimin; Chorev, Michael; Aktas, Bertal H. published 《Development of 1-((1,4-trans)-4-Aryloxycyclohexyl)-3-arylurea Activators of Heme-Regulated Inhibitor as Selective Activators of the Eukaryotic Initiation Factor 2 Alpha (eIF2α) Phosphorylation Arm of the Integrated Endoplasmic Reticulum Stress Response》.Journal of Medicinal Chemistry published the findings.Application of 27489-62-9 The information in the text is summarized as follows:
Heme-regulated inhibitor (HRI), an eukaryotic translation initiation factor 2 alpha (eIF2α) kinase, plays critical roles in cell proliferation, differentiation, adaptation to stress, and Hb disorders. HRI phosphorylates eIF2α that couples cellular signals including the endoplasmic reticulum (ER) stress to translation. The authors 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 arm of ER-stress response as mol. probes for studying HRI biol. and its potential as a druggable target. To develop drug-like cHAUs needed for in vivo studies the authors undertook bioassay guided structure-activity relationship studies and tested them in the surrogate eIF2α phosphorylation and cell proliferation assays. The authors further evaluated some of these cHAUs in endogenous eIF2α phosphorylation and expression of the transcription factor CHOP protein and mRNA demonstrating significantly improved solubility and/or potencies. These cHAUs are excellent candidates for lead optimization for development of investigational new drugs that potently and specifically activate HRI. In the part of experimental materials, we found many familiar compounds, such as trans-4-Aminocyclohexanol(cas: 27489-62-9Application of 27489-62-9)
trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Aniline, ethanolamines, and several other amines are major industrial commodities used in making rubber, dyes, pharmaceuticals, and synthetic resins and fibres and for a host of other applications. Most of the numerous methods for the preparation of amines may be broadly divided into two groups: (1) chemical reduction (replacement of oxygen with hydrogen atoms in the molecule) of members of several other classes of organic nitrogen compounds and (2) reactions of ammonia or amines with organic compounds.Application of 27489-62-9
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