Small molecules inhibit the interaction of Nrf2 and the Keap1 Kelch domain through a non-covalent mechanism

Bioorganic and Medicinal Chemistry

Volumn 21, Issue 14, 2013, Pages 4011-4019

  Marcotte, Douglas ^a   Zeng, Weike ^a   Hus, Jean Christophe ^a   McKenzie, Andres ^a   Hession, Cathy ^a   Jin, Ping ^a   Bergeron, Chris ^a   Lugovskoy, Alexey ^a,d   Enyedy, Istvan ^a   Cuervo, Hernan ^a,e   Wang, Deping ^a   Atmanene, Cédric ^b   Roecklin, Dominique ^b   Vecchi, Malgorzata ^a   Vivat, Valérie ^b   Kraemer, Joachim ^c   Winkler, Dirk ^c   Hong, Victor ^a,f   Chao, Jianhua ^a   Lukashev, Matvey ^a   Silvian, Laura ^a   more..

^a BIOGEN   (United States)

^b NovAliX   (France)

^c EVOTEC AG   (Germany)

^d MERRIMACK PHARMACEUTICALS   (United States)

^e CELGENE CORPORATION   (United States)

^f Keimyung University   (South Korea)

Author keywords

ESI MS; Keap1; Nrf2; Oxidative stress; Protein protein interaction inhibitor; X ray crystallography

Indexed keywords

2 [[5 [(2,5 DIMETHYLBENZENE)SULFONYL] 6 OXO 1,6 DIHYDROPYRIMIDIN 2 YL]SULFANYL] N [2 (TRIFLUOROMETHYL)PHENYL]ACETAMIDE; CPD 15; CPD 16; KELCH LIKE ECH ASSOCIATED PROTEIN 1; N,N' 1,4 NAPHTHALENEDIYLBIS (4 METHOXYBENZENESULFONAMIDE); PROTEIN INHIBITOR; TRANSCRIPTION FACTOR NRF2; UNCLASSIFIED DRUG;

ANTIOXIDANT RESPONSIVE ELEMENT; ARTICLE; BINDING SITE; COMPLEX FORMATION; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG IDENTIFICATION; DRUG STRUCTURE; LIGAND BINDING; MASS SPECTROMETRY; NUCLEAR MAGNETIC RESONANCE; OXIDATION; PROTEIN BINDING; PROTEIN MODIFICATION; PROTEIN PROTEIN INTERACTION; PROTEIN STABILITY; STOICHIOMETRY; STRUCTURE ACTIVITY RELATION; UPREGULATION; X RAY CRYSTALLOGRAPHY;

CARRIER PROTEINS; CRYSTALLOGRAPHY, X-RAY; INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS; NF-E2-RELATED FACTOR 2; PROTEIN BINDING; PROTEIN STRUCTURE, TERTIARY; SMALL MOLECULE LIBRARIES; SPECTROMETRY, MASS, ELECTROSPRAY IONIZATION; STRUCTURE-ACTIVITY RELATIONSHIP; THERMODYNAMICS;

EID: 84879017773     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2013.04.019     Document Type: Article

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