DDRGK1 Enhances Osteosarcoma Chemoresistance via Inhibiting KEAP1‐Mediated NRF2 Ubiquitination
Sign Up to like & getrecommendations! Published in 2023 at "Advanced Science"
DOI: 10.1002/advs.202204438
Abstract: Chemoresistance is the main obstacle in osteosarcoma (OS) treatment; however, the underlying mechanism remains unclear. In this study, it is discovered that DDRGK domain‐containing protein 1 (DDRGK1) plays a fundamental role in chemoresistance induced in… read more here.
Keywords: ddrgk1; ddrgk1 knockout; keap1; enhances osteosarcoma ... See more keywords
MicroRNA‐1225 activates Keap1‐Nrf2‐HO‐1 signalling to inhibit TNFα‐induced osteoclastogenesis by mediating ROS generation
Sign Up to like & getrecommendations! Published in 2019 at "Cell Biochemistry and Function"
DOI: 10.1002/cbf.3394
Abstract: The influence of miRNA‐1225‐5p (miR‐1225) and Keap1‐Nrf2 signalling on in vitro osteoclast differentiation in mouse models was studied along with the underlying mechanism. In differentiated bone marrow–derived macrophages (BMMs), downregulated miR‐1225 and upregulated Keap1 were… read more here.
Keywords: mir 1225; tnf; keap1 nrf2; ros generation ... See more keywords
Diosmetin alleviates cerebral ischemia‐reperfusion injury through Keap1‐mediated Nrf2/ARE signaling pathway activation and NLRP3 inflammasome inhibition
Sign Up to like & getrecommendations! Published in 2022 at "Environmental Toxicology"
DOI: 10.1002/tox.23504
Abstract: Diosmetin was found to exert protective effect on renal and myocardial ischemia‐reperfusion (IR) injury. This study aimed to investigate the role of diosmetin in cerebral IR (CIR) injury. PC12 neurons were exposed to oxygen–glucose deprivation/reoxygenation… read more here.
Keywords: inhibition; diosmetin; keap1; injury ... See more keywords
Identification of potential andrographolide-based drug candidate against Keap1-Nrf2 pathway through rigorous cheminformatics screening.
Sign Up to like & getrecommendations! Published in 2022 at "Molecular diversity"
DOI: 10.1007/s11030-022-10435-3
Abstract: The Keap1-Nrf2 [Kelch-like ECH-associated protein-1-Nuclear factor erythroid-2-related factor-2] regulatory pathway plays a vital role in the protection of cells by regulating transcription of antioxidant and detoxification genes. Andrographolide (AGP) regulates the Keap1-Nrf2 pathway by inhibiting… read more here.
Keywords: keap1 protein; agp; drug; nrf2 pathway ... See more keywords
Suppressed ubiquitination of Nrf2 by p47phox contributes to Nrf2 activation
Sign Up to like & getrecommendations! Published in 2017 at "Free Radical Biology and Medicine"
DOI: 10.1016/j.freeradbiomed.2017.09.011
Abstract: Abstract Although critical in phagocytosis in innate immunity, reactive oxygen species (ROS) collaterally inflict damage to host phagocytes because they indiscriminate targets. Since Nrf2 increases the expression of anti‐oxidant enzymes that nullifies ROS, ROS activating… read more here.
Keywords: ubiquitination nrf2; p47phox; nrf2 p47phox; expression ... See more keywords
Treatment of Dilated Cardiomyopathy in a Mouse Model of Friedreich's Ataxia using N-acetylcysteine and Identification of Alterations in MicroRNA Expression that Could be Involved in its Pathogenesis.
Sign Up to like & getrecommendations! Published in 2020 at "Pharmacological research"
DOI: 10.1016/j.phrs.2020.104994
Abstract: Deficient expression of the mitochondrial protein, frataxin, leads to a deadly cardiomyopathy. Our laboratory reported the master regulator of oxidative stress, nuclear factor erythroid 2-related factor-2 (Nrf2), demonstrates marked down-regulation after frataxin deletion in the… read more here.
Keywords: frataxin; mouse model; expression; keap1 ... See more keywords
Inhibition of TXNRD or SOD1 overcomes NRF2-mediated resistance to β-lapachone
Sign Up to like & getrecommendations! Published in 2020 at "Redox Biology"
DOI: 10.1016/j.redox.2020.101440
Abstract: Alterations in the NRF2/KEAP1 pathway result in the constitutive activation of NRF2, leading to the aberrant induction of antioxidant and detoxification enzymes, including NQO1. The NQO1 bioactivatable agent β-lapachone can target cells with high NQO1… read more here.
Keywords: sod1; lapachone; inhibition; resistance lapachone ... See more keywords
Fragment-Guided Discovery of Pyrazole Carboxylic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2 Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01351
Abstract: The NRF2-mediated cytoprotective response is central to cellular homoeostasis, and there is increasing interest in developing small-molecule activators of this pathway as therapeutics for diseases involving chronic oxidative stress. The protein KEAP1, which regulates NRF2,… read more here.
Keywords: protein; protein interaction; protein protein; keap1 ... See more keywords
Importance of Binding Site Hydration and Flexibility Revealed When Optimizing a Macrocyclic Inhibitor of the Keap1–Nrf2 Protein–Protein Interaction
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.1c01975
Abstract: Upregulation of the transcription factor Nrf2 by inhibition of the interaction with its negative regulator Keap1 constitutes an opportunity for the treatment of disease caused by oxidative stress. We report a structurally unique series of… read more here.
Keywords: interaction; keap1; binding site; hydration flexibility ... See more keywords
Development of Noncovalent Small-Molecule Keap1-Nrf2 Inhibitors by Fragment-Based Drug Discovery.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00830
Abstract: Targeting the protein-protein interaction (PPI) between the transcription factor nuclear factor erythroid 2-related factor 2 (Nrf2) and its repressor, Kelch-like ECH-associated protein 1 (Keap1), constitutes a promising strategy for treating diseases involving oxidative stress and… read more here.
Keywords: drug discovery; small molecule; keap1 nrf2; keap1 ... See more keywords
An Integrated Molecular Grafting Approach for the Design of Keap1-Targeted Peptide Inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "ACS chemical biology"
DOI: 10.1021/acschembio.1c00388
Abstract: Inhibiting the Nrf2:Keap1 interaction to trigger cytoprotective gene expression is a promising treatment strategy for oxidative stress-related diseases. A short linear motif from Nrf2 has the potential to directly inhibit this protein-protein interaction, but poor… read more here.
Keywords: keap1 targeted; molecular grafting; integrated molecular; keap1 ... See more keywords