NRF2 activator 
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  • ||||||||||  Journal:  Mini-GAGR, an intranasally applied polysaccharide, activates the neuronal Nrf2-mediated antioxidant defense system. (Pubmed Central) -  Jun 26, 2019   
    Finally, 20-day intranasal treatment of 3xTg-AD mice with 100 nmole mini-GAGR increased nuclear p-Nrf2 and growth-associated protein 43 (GAP43) levels in hippocampal neurons, reduced p-tau and amyloid-β (Aβ) peptide-stained neurons, and improved memory. The BBB-bypassing Nrf2-activating polysaccharide reported here may be effective in reducing oxidative stress and neurodegeneration in AD.
  • ||||||||||  low molecular weight dextran sulfate (ILB) / TikoMed
    Journal:  Mkp-1 is required for chemopreventive activity of butylated hydroxyanisole and resveratrol against colitis-associated colon tumorigenesis. (Pubmed Central) -  Jun 26, 2019   
    ...In an azoxymethane/dextran sulfate sodium model of colitis-associated tumorigenesis, Mkp-1 mice exhibited a phenotype similar to Nrf2 mice with significantly more tumors than WT mice...In adenomas from WT mice, the expression of Mkp-1 was markedly lower than in adjacent normal tissue, concomitant with the down-regulation of Nrf2 and its target genes. Our data revealed that Mkp-1 is required in the protective role of Nrf2 signaling against colitis-associated tumorigenesis.
  • ||||||||||  Journal:  Lignan and flavonoid support the prevention of cinnamon against oxidative stress related diseases. (Pubmed Central) -  Jun 19, 2019   
    These findings provide insight into PF pathogenesis and a basis for novel treatment approaches. The lignan PRO and the flavonoid MFO are two novel Nrf2 activators protecting tissues against oxidative insults, and these two constituents support the application of cinnamon as an agent against oxidative stress related diseases.
  • ||||||||||  Review, Journal:  The role of Nrf2 signaling in counteracting neurodegenerative diseases. (Pubmed Central) -  Jun 9, 2019   
    Small molecule pharmacological activators of Nrf2 have shown protective effects in numerous animal models of neurodegenerative diseases, and in cultures of human cells expressing mutant proteins. Targeting Nrf2 signaling may provide a therapeutic option to delay onset, slow progression, and ameliorate symptoms of neurodegenerative disorders.
  • ||||||||||  Journal:  Activation of Nrf2 and Hypoxic Adaptive Response Contribute to Neuroprotection Elicited by Phenylhydroxamic Acid Selective HDAC6 Inhibitors. (Pubmed Central) -  May 24, 2019   
    Two superior tripartite agents, ING-6 and ING-66, showed neuroprotection against various cellular insults, associated with stabilization of both Nrf2 and HIF-1, and expression of their respective target genes in vitro and in vivo. Discovery of the innate ability of phenylhydroxamate HDAC inhibitors to activate Nrf2 and HIF provides a novel route to multifunctional neuroprotective agents and cautions against HDAC6 selective inhibitors as chemical probes of specific HDAC isoform function.
  • ||||||||||  Tecfidera (dimethyl fumarate) / Biogen, Fumaderm (dimethyl fumarate) / Biogen
    Preclinical, Journal:  Dimethyl fumarate and vitamin D derivatives cooperatively enhance VDR and Nrf2 signaling in differentiating AML cells in vitro and inhibit leukemia progression in a xenograft mouse model. (Pubmed Central) -  May 24, 2019   
    ...Particularly, dimethyl fumarate (DMF), which is clinically approved for the treatment of multiple sclerosis and psoriasis, strongly cooperated with 1,25D3, PRI-5100 (19-nor-1,25D2; paricalcitol) and PRI-5202 (a double-point modified 19-nor analog of 1,25D2)...Importantly, using a xenograft mouse model we demonstrated that co-administration of PRI-5202 and DMF resulted in a marked cooperative inhibition of human AML tumor growth without inducing treatment toxicity. Collectively, our findings provide a rationale for clinical testing of low-toxic VDD/DMF combinations as a novel approach for differentiation therapy of AML.
  • ||||||||||  Tecfidera (dimethyl fumarate) / Biogen
    Journal:  Aberrant regulation of the GSK-3β/NRF2 axis unveils a novel therapy for adrenoleukodystrophy. (Pubmed Central) -  Apr 28, 2019   
    We find that GSK-3β inhibitors can significantly reactivate the blunted NRF2 response in patients' fibroblasts. In the mouse models (Abcd1 and Abcd1/Abcd2 mice), oral administration of dimethyl fumarate (DMF/BG12/Tecfidera), an NRF2 activator in use for multiple sclerosis, normalized (i) mitochondrial depletion, (ii) bioenergetic failure, (iii) oxidative damage, and (iv) inflammation, highlighting an intricate cross-talk governing energetic and redox homeostasis in X-ALD Importantly, DMF halted axonal degeneration and locomotor disability suggesting that therapies activating NRF2 hold therapeutic potential for X-ALD and other axonopathies with impaired GSK-3β/NRF2 axis.
  • ||||||||||  Journal:  Nrf2 activator for the treatment of kidney diseases. (Pubmed Central) -  Apr 28, 2019   
    The Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2 (Keap1-Nrf2) system has drawn much attention in recent years for its anti-oxidative and anti-inflammatory properties, and its pHarmacological potential for treatment of kidney diseases is being widely investigated in both clinical and non-clinical studies. This review summarizes the current issues in the treatment of kidney diseases, including clinical endpoints, Nrf2 activators as treatment options, and perspectives on pharmaceutical applications of Nrf2 activators.
  • ||||||||||  Journal:  Myocardial NADPH oxidase-4 regulates the physiological response to acute exercise. (Pubmed Central) -  Apr 23, 2019   
    Supplementation with an Nrf2 activator or a mitochondria-targeted antioxidant effectively restores cardiac performance and exercise capacity in csNox4KO and csNrf2KO mice respectively. The Nox4/Nrf2 axis therefore drives a hormetic response that is required for optimal cardiac mitochondrial and contractile function during physiological exercise.
  • ||||||||||  Tecfidera (dimethyl fumarate) / Biogen
    Journal:  Electrophiles modulate glutathione reductase activity via alkylation and upregulation of glutathione biosynthesis. (Pubmed Central) -  Apr 5, 2019   
    In vitro assays in which GR was treated with increasing GSH concentrations and GSH depletion experiments in cells revealed that GR activity is finely regulated via product inhibition, an observation further supported by theoretical (kinetic modeling of cellular GSSG:GSH levels) approaches. Together, these results describe two independent mechanisms by which electrophiles modulate the GSH/GSSG couple, and provide a novel conceptual framework to interpret experimentally determined values of GSH and GSSG.
  • ||||||||||  Journal:  Nuclear trapping of inactive FOXO1 by the Nrf2 activator diethyl maleate. (Pubmed Central) -  Apr 3, 2019   
    Different from FOXO-dependent expression of genes, Nrf2 target gene mRNAs were elevated upon exposure to DEM. These data suggest that, different from C. elegans, DEM elicits opposing effects on the two stress-responsive transcription factors, Nrf2 and FOXO1, in cultured human cells.
  • ||||||||||  Journal:  Neuroprotection of quercetin on central neurons against chronic high glucose through enhancement of Nrf2/ARE/glyoxalase-1 pathway mediated by phosphorylation regulation. (Pubmed Central) -  Apr 3, 2019   
    Moreover, Nrf2/ARE pathway was activated after pretreatment with a PKC activator, p38 MAPK inhibitor, or GSK-3β inhibitor under the condition of HG, and quercetin addition further strengthened this pathway; however, PKC inhibition or GSK-3β activation pretreatment reversed the effects of quercetin on the protein expression of γ-GCS in the HG condition. In summary, quercetin exerts the neuroprotection by enhancing Glo-1 functions in central neurons under chronic HG condition, which may be mediated by activation of Nrf2/ARE pathway; furthermore, the increased Nrf2 phosphorylation mediated by PKC activation and/or GSK-3β inhibition may involve in the activation of Nrf2/ARE pathway.
  • ||||||||||  Journal:  Direct Keap1-Nrf2 disruption as a potential therapeutic target for Alzheimer's disease. (Pubmed Central) -  Mar 23, 2019   
    A new direct inhibitor of the Keap1-Nrf2 binding domain also prevented synaptotoxicity mediated by naturally-derived Aβ oligomers in mouse cortical neurons. Overall, our findings highlight Keap1 specifically as an efficient target for the re-activation of Nrf2 in AD, and support the further investigation of direct Keap1 inhibitors for the prevention of neurodegeneration in vivo.
  • ||||||||||  Tecfidera (dimethyl fumarate) / Biogen
    Preclinical, Journal:  HYCO-3, a dual CO-releaser/Nrf2 activator, reduces tissue inflammation in mice challenged with lipopolysaccharide. (Pubmed Central) -  Mar 23, 2019   
    Furthermore, HYCO-3 diminished TNF-α and IL-1β in brain and liver but not in lung and heart of Nrf2 mice, indicating that the CO-releasing part of this hybrid contributes to reduction of pro-inflammation and that this effect is organ-specific. These data demonstrate that the dual activity of HYCO-3 results in enhanced efficacy compared to the parent compounds indicating the potential exploitation of hybrid compounds in the development of effective anti-inflammatory therapies.
  • ||||||||||  Trial completion, Trial primary completion date:  Effect of Sulforaphane in Broccoli Sprouts on Nrf2 Activation (clinicaltrials.gov) -  May 29, 2015   
    P=N/A,  N=15, Completed, 
    These data demonstrate that the dual activity of HYCO-3 results in enhanced efficacy compared to the parent compounds indicating the potential exploitation of hybrid compounds in the development of effective anti-inflammatory therapies. Active, not recruiting --> Completed | Trial primary completion date: Sep 2011 --> Feb 2013
  • ||||||||||  ITC-6146RO / IntoCell
    Trial completion, Enrollment change, Trial primary completion date:  Effect of Broccoli Sprouts Homogenate on SS RBC (clinicaltrials.gov) -  May 28, 2015   
    P=N/A,  N=21, Completed, 
    Active, not recruiting --> Completed | Trial primary completion date: Sep 2011 --> Feb 2013 Recruiting --> Completed | N=65 --> 21 | Trial primary completion date: Sep 2015 --> Apr 2015
  • ||||||||||  ITC-6146RO / IntoCell
    Trial primary completion date:  Effect of Broccoli Sprouts Homogenate on SS RBC (clinicaltrials.gov) -  Feb 9, 2015   
    P=N/A,  N=65, Recruiting, 
    Recruiting --> Completed | N=65 --> 21 | Trial primary completion date: Sep 2015 --> Apr 2015 Trial primary completion date: Mar 2015 --> Sep 2015
  • ||||||||||  Enrollment open:  Effect of Broccoli Sprouts Homogenate on SS RBC (clinicaltrials.gov) -  Oct 23, 2012   
    P=N/A,  N=65, Recruiting, 
    Trial primary completion date: Mar 2015 --> Sep 2015 Not yet recruiting --> Recruiting