title: Identification and Structural Analysis of New Nrf2 Activators by Mechanism-Based Chemical Transformation of 15-Deoxy-Δ12, 14-PGJ2.
abstract: Mechanism-based chemical transformation of 15-deoxy-Δ12, 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.
authors.affiliation: College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul, 151-742, Republic of Korea.
authors.forename: Kyeojin
authors.initials: K
authors.lastname: Kim
authors.affiliation: CHA Cancer Prevention Research Center, CHA University School of Medicine, Seoul, 135-081, Republic of Korea.
authors.forename: Jong-Min
authors.initials: JM
authors.lastname: Park
authors.affiliation: Department of Pharmacy, College of Pharmacy, Kyung Hee University, 26, Kyungheedae-ro, Dongdaemun-gu, Seoul, 130-701, Republic of Korea.
authors.forename: Nam-Jung
authors.initials: NJ
authors.lastname: Kim
authors.affiliation: Tumor Microenvironment Global Core Research Center, College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul, 151-742, Republic of Korea.
authors.forename: Su-Jung
authors.initials: SJ
authors.lastname: Kim
authors.affiliation: College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul, 151-742, Republic of Korea.
authors.forename: Hyunyoung
authors.initials: H
authors.lastname: Moon
authors.affiliation: College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul, 151-742, Republic of Korea.
authors.forename: Hongchan
authors.initials: H
authors.lastname: An
authors.affiliation: College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul, 151-742, Republic of Korea.
authors.forename: Jeeyeon
authors.initials: J
authors.lastname: Lee
authors.affiliation: School of Pharmacy, Sungkyunkwan University, Suwon, 440-746, Republic of Korea.
authors.forename: Hyun-Ju
authors.initials: HJ
authors.lastname: Park
authors.affiliation: Tumor Microenvironment Global Core Research Center, College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul, 151-742, Republic of Korea. surh@plaza.snu.ac.kr.
authors.forename: Young-Joon
authors.initials: YJ
authors.lastname: Surh
authors.affiliation: College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul, 151-742, Republic of Korea. ygsuh@snu.ac.kr.
authors.forename: Young-Ger
authors.initials: YG
authors.lastname: Suh
mesh_terms: D001665:Binding Sites / Q000187:drug effects; D045744:Cell Line, Tumor; D051547:Heme Oxygenase-1 / Q000096:biosynthesis*; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D051267:NF-E2-Related Factor 2 / Q000378:metabolism*; D015230:Prostaglandin D2 / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: C477819:15-deoxyprostaglandin J2; D051267:NF-E2-Related Factor 2; C496541:HMOX1 protein, human; D051547:Heme Oxygenase-1; D015230:Prostaglandin D2
keywords: 15 deoxy-PGJ2; Keap1; Michael addition; Nrf2; biomimetic synthesis; chemical approach; inhibitors