AIMC Topic: NF-E2-Related Factor 2

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Identification of novel inhibitors of Keap1/Nrf2 by a promising method combining protein-protein interaction-oriented library and machine learning.

Scientific reports Apr 1, 2021
Protein-protein interactions (PPIs) are prospective but challenging targets for drug discovery, because screening using traditional small-molecule libraries often fails to identify hits. Recently, we developed a PPI-oriented library comprising 12,593...
Molecular Structure Molecular Dynamics Simulation Ligands Protein Interaction Maps Protein Binding Structure-Activity Relationship Small Molecule Libraries Protein Interaction Mapping Kelch-Like ECH-Associated Protein 1 Machine Learning Molecular Docking Simulation Drug Discovery Molecular Conformation Humans NF-E2-Related Factor 2 Binding Sites
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Recapitulating the Binding Affinity of Nrf2 for KEAP1 in a Cyclic Heptapeptide, Guided by NMR, X-ray Crystallography, and Machine Learning.

Journal of the American Chemical Society Mar 8, 2021
Macrocycles, including macrocyclic peptides, have shown promise for targeting challenging protein-protein interactions (PPIs). One PPI of high interest is between Kelch-like ECH-Associated Protein-1 (KEAP1) and Nuclear Factor (Erythroid-derived 2)-li...
Humans Machine Learning Structure-Activity Relationship Crystallography, X-Ray Hydrogen Bonding Peptides Protein Binding Recombinant Proteins Cyclization Kelch-Like ECH-Associated Protein 1 NF-E2-Related Factor 2 Mutagenesis, Site-Directed Amino Acid Motifs Fluorescence Polarization Nuclear Magnetic Resonance, Biomolecular
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RASPELD to Perform High-End Screening in an Academic Environment toward the Development of Cancer Therapeutics.

ChemMedChem Aug 23, 2018
The identification of compounds for dissecting biological functions and the development of novel drug molecules are central tasks that often require screening campaigns. However, the required architecture is cost- and time-intensive. Herein we descri...
Kelch-Like ECH-Associated Protein 1 NF-E2-Related Factor 2 Small Molecule Libraries Education, Graduate Mutation Drug Evaluation, Preclinical Biological Assay Ligands ErbB Receptors Protein Kinase Inhibitors Protein Binding Dose-Response Relationship, Drug Robotics Humans Antineoplastic Agents
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Hericium erinaceus Inhibits TNF-α-Induced Angiogenesis and ROS Generation through Suppression of MMP-9/NF-κB Signaling and Activation of Nrf2-Mediated Antioxidant Genes in Human EA.hy926 Endothelial Cells.

Oxidative medicine and cellular longevity Dec 28, 2015
Hericium erinaceus (HE) is an edible mushroom that has been shown to exhibit anticancer and anti-inflammatory activities. We investigated the antiangiogenic and antioxidant potentials of ethanol extracts of HE in human endothelial (EA.hy926) cells up...
Humans Tumor Necrosis Factor-alpha Antioxidants Inflammation Signal Transduction Heme Oxygenase-1 Matrix Metalloproteinase 9 Angiogenesis Inhibitors Reactive Oxygen Species Endothelial Cells Glutathione Intercellular Adhesion Molecule-1 NF-kappa B NF-E2-Related Factor 2 Neovascularization, Pathologic Basidiomycota Anti-Inflammatory Agents Angiogenesis Inducing Agents
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Morin enhances hepatic Nrf2 expression in a liver fibrosis rat model.

World journal of gastroenterology Dec 21, 2017
AIM: To investigate whether morin can reduce hepatic fibrosis by activating the NF-E2-related factor 2 (Nrf2) signaling pathway.
Liver Function Tests Male Antioxidants Carbon Tetrachloride Weight Loss Rats Humans Liver NF-E2-Related Factor 2 Signal Transduction Oxidative Stress Liver Cirrhosis Animals Protective Agents Flavonoids Rats, Sprague-Dawley Disease Models, Animal
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[Effects of hydrogen rich water on the expression of Nrf 2 and the oxidative stress in rats with traumatic brain injury].

Zhonghua wei zhong bing ji jiu yi xue Nov 1, 2015
OBJECTIVE: To investigate the effects of hydrogen rich water on the expression of nuclear factor erythroid 2-related factor 2 (Nrf2) and oxidative stress in rats with traumatic brain injury (TBI).
Random Allocation Hydrogen NF-E2-Related Factor 2 Rats, Sprague-Dawley Brain Injuries Water Oxidative Stress Brain Rats Animals Male
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