Identification and Structural Analysis of New Nrf2 Activators by Mechanism‐Based Chemical Transformation of 15‐Deoxy‐Δ12,  14‐PGJ2. (24th August 2016)

• Record Type: Journal Article
• Authors: Kim, Kyeojin; Park, Jong‐Min; Kim, Nam‐Jung; Kim, Su‐Jung; Moon, Hyunyoung; An, Hongchan; Lee, Jeeyeon; Park, Hyun‐Ju; Surh, Young‐Joon; Suh, Young‐Ger
• Is Part Of: Chembiochem. Volume 17:Number 20(2016)
• Page Start: 1900
• Page End: 1904
• Publication Date: 2016-08-24
• Subjects: 15 deoxy-PGJ2 -- biomimetic synthesis -- chemical approach -- inhibitors -- Keap1 -- Michael addition -- Nrf2; Biochemistry -- Periodicals; Molecular biology -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1002/cbic.201600165
• Languages: English
• ISSNs: 1439-4227

Abstract

Abstract: Mechanism‐based chemical transformation of 15‐deoxy‐Δ 12, 14 ‐PGJ2 (15d‐PGJ2 ) resulted in a series of new NF‐E2‐related factor‐2 (Nrf2) activators and detailed elucidation of the function of each electrophilic binding site. In addition, HO‐1 expression resulting from Nrf2 activation through enhanced dissociation of the Keap1–Nrf2 complex by the new activators was proved. Abstract : Mechanism‐based chemical transformation of 15d‐PGJ2 afforded a series of new Nrf2 activators and allowed detailed elucidation of the function of each electrophilic binding site. HO‐1 expression resulting from the Nrf2 activation through the dissociation enhancement of the Keap1–Nrf2 complex by these activators was proved.