NRF2 activator 
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  • ||||||||||  Review, Journal:  An Overview of NRF2-Activating Compounds Bearing α,β-Unsaturated Moiety and Their Antioxidant Effects. (Pubmed Central) -  Aug 22, 2022   
    This review provides an overview of the reaction mechanism of α,β-unsaturated moiety-bearing compounds with the NRF2/KEAP1 complex, their pharmacological properties, structural activity-relationship and their effect on antioxidant and anti-inflammatory responses. As the first of its kind, this review article offers collective and comprehensive information on NRF2-activators containing α,β-unsaturated moiety with the aim of broadening their therapeutic prospects in a wide range of oxidative stress-related diseases.
  • ||||||||||  Journal:  Anti-Inflammatory Effects of Auranamide and Patriscabratine-Mechanisms and In Silico Studies. (Pubmed Central) -  Aug 22, 2022   
    The possible molecular targets of NRF2 activation by these two compounds were predicted using molecular docking studies and it was found that the compounds might inhibit the Kelch domain of KEAP1 and GSK-3β activity. The physicochemical and drug-like properties of the test compounds were predicted using Schrodinger small molecule drug discovery suite (v.2022-2).
  • ||||||||||  losartan / Generic mfg.
    Preclinical, Journal:  Ginsenoside Re attenuates memory impairments in aged Klotho deficient mice via interactive modulations of angiotensin II AT1 receptor, Nrf2 and GPx-1 gene. (Pubmed Central) -  Aug 18, 2022   
    Both GRe and the AT1 receptor antagonist losartan failed to attenuate the decrease in phosphorylation of JAK2/STAT3 in aged Klotho deficient (±) mice but significantly activated nuclear factor erythroid 2-related factor 2 (Nrf2)-mediated signaling...Both the GPx inhibitor mercaptosuccinate and Nrf2 inhibitor brusatol counteracted the effects of GRe on all neurobehavioral impairments in aged Klotho deficient (±) mice. Our results suggest that GRe attenuates all alterations, such as AT1 receptor expression, NOX-, ROS-, and GPx-levels, and cognitive dysfunction in aged Klotho deficient (±) mice via upregulation of Nrf2/GPx-1/ERK/CREB signaling.
  • ||||||||||  Journal:  Nrf2 as a regulator of mitochondrial function: Energy metabolism and beyond. (Pubmed Central) -  Aug 18, 2022   
    We focus on Nrf2 involvement in promoting mitochondrial quality control and regulation of basic aspects of mitochondrial function, including energy production, reactive oxygen species generation, calcium signalling, and cell death induction. Given the importance of mitochondria in the development of multiple diseases, these findings reinforce the pharmacological activation of Nrf2 as an attractive strategy to counteract mitochondrial dysfunction.
  • ||||||||||  SP600125 / BMS
    Preclinical, Journal:  Carveol ameliorates mercury-induced oxidative stress, neuroinflammation, and neurodegeneration in a mouse brain. (Pubmed Central) -  Aug 14, 2022   
    Taken together, these data suggest that GPF reduces H. pylori-induced gastric mucosa injury by activating Nrf2 signaling and that GPF is a potential candidate for the treatment of H. pylori-associated gastritis. Our findings indicate that carveol can inhibit the p-JNK pathway, thereby inhibiting HgCl2-induced apoptosis and downregulating the expression of inflammatory mediators.
  • ||||||||||  Review, Journal:  A mechanistic review on immunomodulatory effects of selective type two cannabinoid receptor β-caryophyllene. (Pubmed Central) -  Aug 14, 2022   
    Previous results indicated that the antioxidant effects of β-caryophyllene were suggested through different pathways, including activation of nuclear factor erythroid 2-related factor-2 (Nrf2)/heme oxygenase-1 (HO-1)/antioxidant axis and inhibition of the HMG-CoA reductase activity, and oxidative stress biomarkers levels. Furthermore, various results showed immunomodulatory effects of BCP through inhibiting microglial cells, CD and CD T lymphocytes, modulated Th /T immune balance through the activation of the CB receptor, and reducing mitogen-activated protein kinases (p38MAPK) and NF-kB activation and increased ionized calcium-binding adaptor molecule-1 (Iba-1) and IL-1β.
  • ||||||||||  cisplatin / Generic mfg.
    Journal:  Quercetin Mitigates Cisplatin-Induced Oxidative Damage and Apoptosis in Cardiomyocytes through Nrf2/HO-1 Signaling Pathway. (Pubmed Central) -  Aug 14, 2022   
    In conclusion, this study reports that quercetin has the potential to antagonize cisplatin-caused cardiotoxicity by reducing ROS-mediated mitochondrial damage and inflammation via the Nrf2/HO-1 and p38MAPK/NF-[Formula: see text]Bp65/IL-8 signaling pathway. This study provided the theoretical basis and experimental proof for the clinical application of quercetin as a new effective strategy to relieve chemotherapy-induced cardiotoxicity.
  • ||||||||||  Oxidative Damage is a Hallmark of Atopic Dermatitis in Humans and Mice (Room 1) -  Aug 11, 2022 - Abstract #ESDR2022ESDR_22;    
    Both features are aggravated by additional loss of Nrf2, suggesting a role of oxidative stress in the phenotype. Together, these results identify a potential role of an impaired Nrf2-mediated oxidative stress response in chronic skin inflammation, which could be therapeutically explored in AD patients.
  • ||||||||||  Review, Journal:  Flexion of Nrf2 by tea phytochemicals: A review on the chemopreventive and chemotherapeutic implications. (Pubmed Central) -  Aug 11, 2022   
    Tea catechins show their dual Nrf2-modulatory effect by directly acting on Nrf2-Keap1 or their upstream regulators and downstream effectors in a highly case-specific manner. In this review, we have tried to present a comprehensive evaluation of the Nrf2-mediated chemopreventive and chemotherapeutic applications of tea in various preclinical cancer models, the Nrf2-modulatory mechanisms, and the limitations which need to be addressed in future research.
  • ||||||||||  selenomethionine (SLM) / University of Iowa, Holden Comprehensive Cancer Center
    Preclinical, Journal:  SeMet attenuates AFB1-induced intestinal injury in rabbits by activating the Nrf2 pathway. (Pubmed Central) -  Aug 10, 2022   
    The aim of this study was to investigate the role of selenomethionine (SeMet) in alleviating AFB1 induced intestinal injury by inhibiting intestinal oxidative stress...SeMet pretreatment significantly improved the performance of the rabbits, alleviated intestinal oxidative stress and the inflammatory response. Therefore, we confirmed that SeMet protects against AFB1 induced oxidative damage and improves productivity in rabbits by activating the Nrf2/HO-1 signaling pathway.
  • ||||||||||  Development of protein-like polymer therapeutics for modulating the Nrf2/Keap1 protein-protein interaction | Poster Board #2871 (Hall F2 (McCormick Place Convention Center)) -  Aug 9, 2022 - Abstract #ACSFall2022ACS_Fall_12924;    
    In summary, we successfully synthesized and characterized a novel biomaterial capable of overcoming the current challenges facing peptide therapeutics by achieving cellular uptake, enhanced binding affinity, and demonstrated bioactivity. This work is a step forward in the development of methods for direct inhibition of intracellular PPIs and has potential for clinical translation.
  • ||||||||||  Synthesis of non-electrophilic, NRF2-activating prodrugs | Poster Board #3471 (Hall F2 (McCormick Place Convention Center)) -  Aug 9, 2022 - Abstract #ACSFall2022ACS_Fall_3432;    
    In an effort to increase cell permeability and lipophilicity of the compound, we have synthesized a series of PRL-295 prodrugs and bioisosteres, which will replace the carboxylic moiety of the original compound. With further testing, we hope to demonstrate improved pharmacological activity.