Published in PLoS One on June 04, 2014
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RTA 408, A Novel Synthetic Triterpenoid with Broad Anticancer and Anti-Inflammatory Activity. PLoS One (2015) 0.86
Prophylactic and therapeutic treatment with a synthetic analogue of a parasitic worm product prevents experimental arthritis and inhibits IL-1β production via NRF2-mediated counter-regulation of the inflammasome. J Autoimmun (2015) 0.84
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Characterization of RA839, a Noncovalent Small Molecule Binder to Keap1 and Selective Activator of Nrf2 Signaling. J Biol Chem (2015) 0.78
Probing the structural requirements of non-electrophilic naphthalene-based Nrf2 activators. Eur J Med Chem (2015) 0.78
Cancer Cell Growth Is Differentially Affected by Constitutive Activation of NRF2 by KEAP1 Deletion and Pharmacological Activation of NRF2 by the Synthetic Triterpenoid, RTA 405. PLoS One (2015) 0.77
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Safety, pharmacokinetics, and pharmacodynamics of oral omaveloxolone (RTA 408), a synthetic triterpenoid, in a first-in-human trial of patients with advanced solid tumors. Onco Targets Ther (2017) 0.75
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Distinct cysteine residues in Keap1 are required for Keap1-dependent ubiquitination of Nrf2 and for stabilization of Nrf2 by chemopreventive agents and oxidative stress. Mol Cell Biol (2003) 6.91
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Oxidative and electrophilic stresses activate Nrf2 through inhibition of ubiquitination activity of Keap1. Mol Cell Biol (2006) 3.97
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Keap1 recruits Neh2 through binding to ETGE and DLG motifs: characterization of the two-site molecular recognition model. Mol Cell Biol (2006) 3.27
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Cellular mechanisms of redox cell signalling: role of cysteine modification in controlling antioxidant defences in response to electrophilic lipid oxidation products. Biochem J (2004) 3.15
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Modifying specific cysteines of the electrophile-sensing human Keap1 protein is insufficient to disrupt binding to the Nrf2 domain Neh2. Proc Natl Acad Sci U S A (2005) 2.92
Structures of SPOP-substrate complexes: insights into molecular architectures of BTB-Cul3 ubiquitin ligases. Mol Cell (2009) 2.84
Two-site substrate recognition model for the Keap1-Nrf2 system: a hinge and latch mechanism. Biol Chem (2006) 2.61
The antioxidant defense system Keap1-Nrf2 comprises a multiple sensing mechanism for responding to a wide range of chemical compounds. Mol Cell Biol (2008) 2.57
Targeting Nrf2 with the triterpenoid CDDO-imidazolide attenuates cigarette smoke-induced emphysema and cardiac dysfunction in mice. Proc Natl Acad Sci U S A (2008) 2.53
The Nrf2/ARE pathway as a potential therapeutic target in neurodegenerative disease. Antioxid Redox Signal (2009) 2.49
Different electrostatic potentials define ETGE and DLG motifs as hinge and latch in oxidative stress response. Mol Cell Biol (2007) 2.38
Specific patterns of electrophile adduction trigger Keap1 ubiquitination and Nrf2 activation. J Biol Chem (2005) 2.37
Identification of sensor cysteines in human Keap1 modified by the cancer chemopreventive agent sulforaphane. Chem Res Toxicol (2005) 2.22
Nrf2-deficient mice are highly susceptible to cigarette smoke-induced emphysema. Genes Cells (2005) 2.18
Physiological significance of reactive cysteine residues of Keap1 in determining Nrf2 activity. Mol Cell Biol (2008) 2.15
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Keap1 perceives stress via three sensors for the endogenous signaling molecules nitric oxide, zinc, and alkenals. Proc Natl Acad Sci U S A (2010) 1.72
Novel n-3 fatty acid oxidation products activate Nrf2 by destabilizing the association between Keap1 and Cullin3. J Biol Chem (2006) 1.70
Retracted Antioxidant-induced modification of INrf2 cysteine 151 and PKC-delta-mediated phosphorylation of Nrf2 serine 40 are both required for stabilization and nuclear translocation of Nrf2 and increased drug resistance. J Cell Sci (2009) 1.58
Activation of the Nrf2-ARE signaling pathway: a promising strategy in cancer prevention. Bioessays (2006) 1.55
The cancer chemopreventive actions of phytochemicals derived from glucosinolates. Eur J Nutr (2008) 1.55
Identification of the highly reactive cysteine 151 in the chemopreventive agent-sensor Keap1 protein is method-dependent. Chem Res Toxicol (2007) 1.53
Keap1 is a forked-stem dimer structure with two large spheres enclosing the intervening, double glycine repeat, and C-terminal domains. Proc Natl Acad Sci U S A (2010) 1.48
Covalent modification at Cys151 dissociates the electrophile sensor Keap1 from the ubiquitin ligase CUL3. Chem Res Toxicol (2008) 1.47
Structural basis for Cul3 protein assembly with the BTB-Kelch family of E3 ubiquitin ligases. J Biol Chem (2013) 1.46
Emerging roles of Nrf2 and phase II antioxidant enzymes in neuroprotection. Prog Neurobiol (2012) 1.41
Adaptor protein self-assembly drives the control of a cullin-RING ubiquitin ligase. Structure (2012) 1.37
Sites of alkylation of human Keap1 by natural chemoprevention agents. J Am Soc Mass Spectrom (2007) 1.36
Targeting the Nrf2 pathway against cardiovascular disease. Expert Opin Ther Targets (2009) 1.28
Dihydro-CDDO-trifluoroethyl amide (dh404), a novel Nrf2 activator, suppresses oxidative stress in cardiomyocytes. PLoS One (2009) 1.24
Validation of the multiple sensor mechanism of the Keap1-Nrf2 system. Free Radic Biol Med (2012) 1.18
Modification of keap1 cysteine residues by sulforaphane. Chem Res Toxicol (2011) 1.17
Automated protein-ligand crystallography for structure-based drug design. ChemMedChem (2006) 1.16
Discovery of an allosteric mechanism for the regulation of HCV NS3 protein function. Nat Chem Biol (2012) 1.13
Chemopreventive promise of targeting the Nrf2 pathway. Drug News Perspect (2007) 1.13
Design, synthesis, and biological evaluation of biotin conjugates of 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid for the isolation of the protein targets. J Med Chem (2004) 1.09
Prospective type 1 and type 2 disulfides of Keap1 protein. Chem Res Toxicol (2008) 1.09
Cul3-mediated Nrf2 ubiquitination and antioxidant response element (ARE) activation are dependent on the partial molar volume at position 151 of Keap1. Biochem J (2009) 1.09
Chiral decalins: preparation from oleanolic acid and application in the synthesis of (-)-9-epi-ambrox. J Nat Prod (2006) 1.04
Crystal structure of KLHL3 in complex with Cullin3. PLoS One (2013) 1.02
Fragment screening using X-ray crystallography. Top Curr Chem (2012) 0.95
Keap calm, and carry on covalently. J Med Chem (2013) 0.87
Insights into strand exchange in BTB domain dimers from the crystal structures of FAZF and Miz1. J Mol Biol (2010) 0.86
Diffusion dynamics of the Keap1-Cullin3 interaction in single live cells. Biochem Biophys Res Commun (2013) 0.83