Characterization of Aminobenzylphenols as Protein Disulfide Isomerase Inhibitors in Glioblastoma Cell Lines was written by Shergalis, Andrea;Xue, Ding;Gharbia, Fatma Z.;Driks, Hannah;Shrestha, Binita;Tanweer, Amina;Cromer, Kirin;Ljungman, Mats;Neamati, Nouri. And the article was included in Journal of Medicinal Chemistry in 2020.Electric Literature of C7H6O3 This article mentions the following:
Disulfide bond formation is a critical post-translational modification of newly synthesized polypeptides in the oxidizing environment of the endoplasmic reticulum and is mediated by protein disulfide isomerase (PDIA1). In this study, we report a series of α-aminobenzylphenol analogs as potent PDI inhibitors. The lead compound, AS15, is a covalent nanomolar inhibitor of PDI, and the combination of AS15 analogs with glutathione synthesis inhibitor buthionine sulfoximine (BSO) leads to synergistic cell growth inhibition. Using nascent RNA sequencing, we show that an AS15 analog triggers the unfolded protein response in glioblastoma cells. A BODIPY-labeled analog binds proteins including PDIA1, suggesting that the compounds are cell-permeable and reach the intended target. Taken together, these findings demonstrate an extensive biochem. characterization of a novel series of highly potent reactive small mols. that covalently bind to PDI. In the experiment, the researchers used many compounds, for example, Benzo[d][1,3]dioxol-4-ol (cas: 69393-72-2Electric Literature of C7H6O3).
Benzo[d][1,3]dioxol-4-ol (cas: 69393-72-2) belongs to alcohols. Alcohols are among the most common organic compounds. They are used as sweeteners and in making perfumes, are valuable intermediates in the synthesis of other compounds, and are among the most abundantly produced organic chemicals in industry. Tertiary alcohols cannot be oxidized at all without breaking carbon-carbon bonds, whereas primary alcohols can be oxidized to aldehydes or further oxidized to carboxylic acids.Electric Literature of C7H6O3
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts