Frenolicin B Targets Peroxiredoxin 1 and Glutaredoxin 3 to Trigger ROS/4E-BP1-Mediated Antitumor Effects was written by Ye, Qing;Zhang, Yinan;Cao, Yanan;Wang, Xiachang;Guo, Yubin;Chen, Jing;Horn, Jamie;Ponomareva, Larissa V.;Chaiswing, Luksana;Shaaban, Khaled A.;Wei, Qiou;Anderson, Bradley D.;St, Clair Daret K.;Zhu, Haining;Leggas, Markos;Thorson, Jon S.;She, Qing-Bai. And the article was included in Cell Chemical Biology in 2019.Product Details of 18080-67-6 This article mentions the following:
Peroxiredoxin 1 (Prx1) and glutaredoxin 3 (Grx3) are two major antioxidant proteins that play a critical role in maintaining redox homeostasis for tumor progression. Here, we identify the prototypical pyranonaphthoquinone natural product frenolicin B (FB) as a selective inhibitor of Prx1 and Grx3 through covalent modification of active-site cysteines. FB-targeted inhibition of Prx1 and Grx3 results in a decrease in cellular glutathione levels, an increase of reactive oxygen species (ROS), and concomitant inhibition of cancer cell growth, largely by activating the peroxisome-bound tuberous sclerosis complex to inhibit mTORC1/4E-BP1 signaling axis. FB structure-activity relationship studies reveal a pos. correlation between inhibition of 4E-BP1 phosphorylation, ROS-mediated cancer cell cytotoxicity, and suppression of tumor growth in vivo. These findings establish FB as the most potent Prx1/Grx3 inhibitor reported to date and also notably highlight 4E-BP1 phosphorylation status as a potential predictive marker in response to ROS-based therapies in cancer. In the experiment, the researchers used many compounds, for example, 2,3-Bis(bromomethyl)quinoxaline 1,4-dioxide (cas: 18080-67-6Product Details of 18080-67-6).
2,3-Bis(bromomethyl)quinoxaline 1,4-dioxide (cas: 18080-67-6) belongs to quinoxaline derivatives. Quinoxaline derivatives are important constituents of pharmacologically active compounds, including as well as for RNA synthesis inhibition, reactive dyes and pigments, azo dyes, flurox Cylin Dyes, Corrosion Inhibitors and Photovoltaic Polymers. They are well-known for application in organic light emitting devices, polymers and pharmaceutical agents. The quinoxaline-containing polymers are applicable in optical devices due to their thermal stability and low band gap.Product Details of 18080-67-6
Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider