Mitoquinone Inactivates Mitochondrial Chaperone TRAP1 by Blocking the Client Binding Site was written by Yoon, Nam Gu;Lee, Hakbong;Kim, So-Yeon;Hu, Sung;Kim, Darong;Yang, Sujae;Hong, Ki Bum;Lee, Ji Hoon;Kang, Soosung;Kim, Byung-Gyu;Myung, Kyungjae;Lee, Changwook;Kang, Byoung Heon. And the article was included in Journal of the American Chemical Society in 2021.Related Products of 605-94-7 This article mentions the following:
Heat shock protein 90 (Hsp90) family proteins are mol. chaperones that modulate the functions of various substrate proteins (clients) implicated in pro-tumorigenic pathways. In this study, the mitochondria-targeted antioxidant mitoquinone (MitoQ) was identified as a potent inhibitor of mitochondrial Hsp90, known as a tumor necrosis factor receptor-associated protein 1 (TRAP1). Structural analyses revealed an asym. bipartite interaction between MitoQ and the previously unrecognized drug binding sites located in the middle domain of TRAP1, believed to be a client binding region. MitoQ effectively competed with TRAP1 clients, and MitoQ treatment facilitated the identification of 103 TRAP1-interacting mitochondrial proteins in cancer cells. MitoQ and its redox-crippled SB-U014/SB-U015 exhibited more potent anticancer activity in vitro and in vivo than previously reported mitochondria-targeted TRAP1 inhibitors. The findings indicate that targeting the client binding site of Hsp90 family proteins offers a novel strategy for the development of potent anticancer drugs. In the experiment, the researchers used many compounds, for example, 2,3-Dimethoxy-5-methylcyclohexa-2,5-diene-1,4-dione (cas: 605-94-7Related Products of 605-94-7).
2,3-Dimethoxy-5-methylcyclohexa-2,5-diene-1,4-dione (cas: 605-94-7) belongs to ethers. The oxygen atom in ethers are more electronegative than carbon, thus the hydrogens which are alpha to the ethers are more acidic than the simple hydrocarbons. The unique properties of ethers (i.e., that they are strongly polar, with nonbonding electron pairs but no hydroxyl group) enhance the formation and use of many reagents. For example, Grignard reagents cannot form unless an ether is present to share its lone pair of electrons with the magnesium atom. Complexation of the magnesium atom stabilizes the Grignard reagent and helps to keep it in solution.Related Products of 605-94-7
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem