NRF2 activator 
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  • ||||||||||  Journal:  COPD lung studies of Nrf2 expression and the effects of Nrf2 activators. (Pubmed Central) -  Jul 23, 2022   
    There is evidence of dysregulation of the Nrf2 signalling pathway in AM from COPD patients. The higher potency of the novel PPI Nrf2 compound C4X_6665 for inducing antioxidant activity and gene expression compared to electrophilic and other PPI Nrf2 activators highlights the therapeutic potential of this compound to address Nrf2 pathway dysregulation in COPD AM.
  • ||||||||||  Journal:  Nrf2 protects against radiation-induced oral mucositis via antioxidation and keratin layer thickening. (Pubmed Central) -  Jul 23, 2022   
    In agreement with the genetic Nrf2 activation model, the Nrf2 inducer CDDO-Im prevented irradiation damage to the tongue epithelium. These results demonstrate that Nrf2 activation has the potential to prevent the development of radiation-induced mucositis and that Nrf2 inducers are an important therapeutic drug for protection of the upper aerodigestive tract from radiation-induced mucositis.
  • ||||||||||  Journal:  AMPK activates the Nrf2-Keap1 pathway to govern dendrite pruning via insulin pathway in Drosophila. (Pubmed Central) -  Jul 20, 2022   
    Moreover, the AMPK-insulin pathway is required for ecdysone signaling to activate Nrf2-Keap1 pathway during dendrite pruning. Overall, this study reveals an important mechanism whereby ecdysone signaling activates Nrf2-Keap1 pathway via the AMPK-insulin pathway to promote dendrite pruning, and further suggests that during the nonfeeding prepupal stage the metabolic alterations lead to activation of Nrf2-Keap1 pathway and dendrite pruning.
  • ||||||||||  cisplatin / Generic mfg., methotrexate / Generic mfg.
    Journal:  Plk2-mediated phosphorylation and translocalization of Nrf2 activates anti-inflammation through p53/Plk2/p21 signaling in acute kidney injury. (Pubmed Central) -  Jul 17, 2022   
    Of note, Plk2 directly phosphorylated Nrf2 at Ser40, which facilitated its interaction with p21 and translocation into the nuclei for the activation of anti-oxidative and anti-inflammatory factors in response to AKI. Together, these findings suggest that Plk2 may serve as an anti-oxidative and anti-inflammatory regulator through the phosphorylation and activation of Nrf2 to protect kidney cells from kidney toxicants and that Plk2 and Nrf2 therefore work cooperatively for the protection and survival of kidney cells from harmful stresses.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  Exosomes from human induced pluripotent stem cells derived mesenchymal stem cells improved myocardial injury caused by severe acute pancreatitis through activating Akt/Nrf2/HO-1 axis. (Pubmed Central) -  Jul 17, 2022   
    Our data indicated that the Exo from iMSCs could improve MI caused by SAP through activating Nrf2/HO-1 axis. These findings firstly unfold the potential application of Exo from iMSCs in treating MI induced by SAP.Abbreviations: LVEF: Left ventricular ejection fraction; LVFS: left ventricular fractional shorten; LVDd: left ventricular end-diastolic diameter; LVDs: left ventricular end-systolic diameter; MI: Myocardial infarction; MSCs: Mesenchymal stem cells; iPSCs: Human-induced pluripotent stem cells; SAP: Severe acute pancreatitis; iMSCs: iPSCs derived VEGF: MSCs; vascular endothelial growth factor; Nrf2: Nuclear factor erythroid 2-related factor; RT-PCR: Real-time polymerase chain reaction; HE: Hematoxylin-eosin; MODS: Multiple organ dysfunction syndrome; PI3K: Phosphatidylinositol 3-kinase; SOD: Superoxide dismutase; FBS: Fetal bovine serum; ECL: Enhanced chemiluminescence; IHC: Immunohistochemistry.
  • ||||||||||  Review, Journal, Tumor Mutational Burden:  State-of-the-Art Molecular Oncology of Lung Cancer in Taiwan. (Pubmed Central) -  Jul 17, 2022   
    The molecular profiling of advanced NSCLC is critical to optimal therapeutic decision-making. The patient characteristics, such as mutation profiles, protein expression profiles, drug-resistance profiles, molecular oncogenic mechanisms and patient subgroup systems together offer new strategies for personalized treatments and patient care.
  • ||||||||||  Journal:  Scutellarin protects the kidney from ischemia/reperfusion injury by targeting Nrf2. (Pubmed Central) -  Jul 16, 2022   
    Our findings indicate that Nrf2 activation and the associated increase in metabolism play roles in ACC, in particular in ACC with a Weiss score of 7 to 9 and a Helsinki score of greater than 17. Scu led to up-regulation of HO-1 through activating the Nrf2 signalling pathway, protecting the kidneys from ischemia/reperfusion (I/R)-induced oxidative damage.
  • ||||||||||  Review, Journal:  Signal amplification in the KEAP1-NRF2-ARE antioxidant response pathway. (Pubmed Central) -  Jul 15, 2022   
    The emergence and degree of ultrasensitivity depend on the strengths of protein-protein and protein-DNA interaction and protein abundances. A unique, quantitative understanding of signal amplification in the KEAP1-NRF2-ARE pathway will help to identify sensitive targets for the prevention and therapeutics of oxidative stress-related diseases and develop quantitative adverse outcome pathway models to facilitate the health risk assessment of oxidative chemicals.
  • ||||||||||  Review, Journal:  Role of Nrf2 in Parkinson's Disease: Toward New Perspectives. (Pubmed Central) -  Jul 13, 2022   
    This review summarized the role of Nrf2 pathway on the pathogenesis of PD. Regulation of Nrf2 pathway might be one of the promising strategies to prevent and treat PD.
  • ||||||||||  lapatinib / Generic mfg.
    Journal:  AF8c, a Multi-Kinase Inhibitor Induces Apoptosis by Activating DR5/Nrf2 via ROS in Colorectal Cancer Cells. (Pubmed Central) -  Jul 11, 2022   
    Our team has previously reported a series of quinazoline-based lapatinib hybrids as potent kinase-targeting anticancer agents...Overall, our results suggest that AF8c-induced apoptosis may be associated with DR5/Nrf2 activation through ER stress and ROS generation in CRC cells. These findings indicate that AF8c represents a promising polypharmacological molecule for the treatment of human CRC.
  • ||||||||||  Journal:  Gamma-oryzanol protects human liver cell (L02) from hydrogen peroxide-induced oxidative damage through regulation of the MAPK/Nrf2 signaling pathways. (Pubmed Central) -  Jul 10, 2022   
    PRACTICAL APPLICATIONS: Gamma-oryzanol (Orz), a mixture of the ferulic acid ester of triterpene alcohols and phytosterols, was found abundantly in rice bran and rice bran oil which could be availably served as an antioxidant. In this study, it was found that Orz exerts the cytoprotective effects in H O -induced L02 cell apoptosis by ameliorating oxidative stress via the inhibition of MAPK signaling pathway and the activation of Nrf2 signaling pathway, which provides a theoretical basis for dietary adding natural products to prevent or treat oxidative stress-related diseases.
  • ||||||||||  RSL3 / Stanford University
    Journal:  Leonurine hydrochloride alleviates ferroptosis in cisplatin-induced acute kidney injury by activating the Nrf2 signaling pathway. (Pubmed Central) -  Jul 10, 2022   
    In this study, it was found that Orz exerts the cytoprotective effects in H O -induced L02 cell apoptosis by ameliorating oxidative stress via the inhibition of MAPK signaling pathway and the activation of Nrf2 signaling pathway, which provides a theoretical basis for dietary adding natural products to prevent or treat oxidative stress-related diseases. These data suggest that renal protective effects of Nrf2 activation on cisplatin-induced acute kidney injury are achieved, at least partially, by inhibiting lipid peroxide-mediated ferroptosis, highlighting the potential of leonurine in acute kidney injury treatment.
  • ||||||||||  liproxstatin-1 / Jilin University
    Journal:  Induction of ferroptosis by carnosic acid-mediated inactivation of Nrf2/HO-1 potentiates cisplatin responsiveness in OSCC cells. (Pubmed Central) -  Jul 9, 2022   
    Treatment with carnosic acid induced ferroptosis in cisplatin-resistant OSCC cells; however, this suppression was reversed following the application of ferroptosis antagonist liproxstatin-1 (Lip-1), indicating the involvement of ferroptosis for carnosic acid-mediated cisplatin resistance...Together, the current findings highlight that carnosic acid may re-sensitize cisplatin-resistant cells to cisplatin by inducing ferroptosis, which involves the inactivation of Nrf2/HO-1/xCT pathway. Hence, this research may support a promising therapeutic approach to overcome chemoresistance in OSCC.
  • ||||||||||  Review, Journal:  Redox and Other Biological Activities of Tea Catechins That May Affect Health: Mechanisms and Unresolved Issues. (Pubmed Central) -  Jul 9, 2022   
    We also review the effects of EGCG on the activities of enzymes, receptors, and other signaling molecules through binding and raise a question about whether the autoxidation of EGCG in vitro may lead to artifacts or misinterpretation in some studies. Finally, we discuss the challenges in the extrapolation of in vitro results to situations in vivo and the translation of laboratory studies to humans.
  • ||||||||||  Review, Journal:  An update of Nrf2 activators and inhibitors in cancer prevention/promotion. (Pubmed Central) -  Jul 9, 2022   
    Taken together, these findings suggest that reaching an optimal balance between paradoxical functions of Nrf2 in malignancy may render a selective improvement to identify therapeutic strategies in cancer treatment. In this review, we describe lately discovered Nrf2 inducers and inhibitors, and their chemopreventive and/or anticancer activities.