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Identification and Structural Analysis of New Nrf2 Activators by Mechanism‐Based Chemical Transformation of 15‐Deoxy‐Δ 12, 14 ‐PGJ 2
Author(s) -
Kim Kyeojin,
Park JongMin,
Kim NamJung,
Kim SuJung,
Moon Hyunyoung,
An Hongchan,
Lee Jeeyeon,
Park HyunJu,
Surh YoungJoon,
Suh YoungGer
Publication year - 2016
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.201600165
Subject(s) - chemistry , electrophile , mechanism (biology) , transformation (genetics) , stereochemistry , combinatorial chemistry , computational biology , biochemistry , biology , physics , quantum mechanics , gene , catalysis
Mechanism‐based chemical transformation of 15‐deoxy‐Δ 12, 14 ‐PGJ 2 (15d‐PGJ 2 ) 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.