A potent phosphodiester Keap1-Nrf2 protein-protein interaction inhibitor as the efficient treatment of Alzheimer's disease

Omaveloxolone: First Approval

(2023) Arnold Lee   DRUGS

Crystallography-Guided Optimizations of the Keap1–Nrf2 Inhibitors on the Solvent Exposed Region: From Symmetric to Asymmetric Naphthalenesulfonamides

(2022) Guodong Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Efficacy of Omaveloxolone in Friedreich's Ataxia: Delayed‐Start Analysis of the MOXIe Extension

(2022) David R. Lynch et al.   MOVEMENT DISORDERS

Mitochondrial Dysfunction and Oxidative Stress in Alzheimer’s Disease

(2021) Afzal Misrani et al.   Frontiers in Aging Neuroscience

Deconstructing Noncovalent Kelch-like ECH-Associated Protein 1 (Keap1) Inhibitors into Fragments to Reconstruct New Potent Compounds

(2021) Jakob S. Pallesen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Molecular basis for the disruption of Keap1–Nrf2 interaction via Hinge & Latch mechanism

(2021) Yuta Horie et al.   Communications Biology

Structure-based molecular hybridization design of Keap1-Nrf2 inhibitors as novel protective agents of acute lung injury

(2021) Le Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Ligand-based substituent-anchoring design of selective receptor-interacting protein kinase 1 necroptosis inhibitors for ulcerative colitis therapy

(2021) Jing Zhu et al.   Acta Pharmaceutica Sinica B

Oxidative stress in the pathogenesis of Alzheimer’s disease and cerebrovascular disease with therapeutic implications.

(2020) Anamaria Jurcau et al.   CNS & Neurological Disorders-Drug Targets

Nrf2 Suppresses Oxidative Stress and Inflammation in App Knock-In Alzheimer’s Disease Model Mice

(2020) Akira Uruno et al.   MOLECULAR AND CELLULAR BIOLOGY

Reactive oxygen species (ROS) as pleiotropic physiological signalling agents

(2020) Helmut Sies et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Nrf2 Ablation Promotes Alzheimer’s Disease-Like Pathology in APP/PS1 Transgenic Mice: The Role of Neuroinflammation and Oxidative Stress

(2020) Peng Ren et al.   Oxidative Medicine and Cellular Longevity

Structural insights into the multiple binding modes of Dimethyl Fumarate (DMF) and its analogs to the Kelch domain of Keap1

(2020) Sruthi Unni et al.   FEBS Journal

Safety and Efficacy of Omaveloxolone in Friedreich's Ataxia ( MOXIe Study)

(2020) David R. Lynch et al.   ANNALS OF NEUROLOGY

Direct inhibition of Keap1-Nrf2 Protein-Protein interaction as a potential therapeutic strategy for Alzheimer's disease

(2020) Yi Sun et al.   BIOORGANIC CHEMISTRY

Recent progress in Keap1-Nrf2 protein-protein interaction inhibitors

(2020) Yi Mou et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of New Tyrosol‐Based Phosphodiester Derivatives: Effect on Amyloid β Aggregation and Metal Chelation Ability

(2020) Valeria Romanucci et al.   ChemMedChem

Therapeutic targeting of the NRF2 and KEAP1 partnership in chronic diseases

(2019) Antonio Cuadrado et al.   NATURE REVIEWS DRUG DISCOVERY

Neuroprotective Effect of Swertiamain on Cerebral Ischemia/Reperfusion Injury by Inducing the Nrf2 Protective Pathway

(2019) Hui Wang et al.   ACS Chemical Neuroscience

NRF2/ARE pathway negatively regulates BACE1 expression and ameliorates cognitive deficits in mouse Alzheimer’s models

(2019) Gahee Bahn et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Fragment-growing guided design of Keap1-Nrf2 protein-protein interaction inhibitors for targeting myocarditis

(2018) Ning Meng et al.   FREE RADICAL BIOLOGY AND MEDICINE

Oxidative Stress, Amyloid-β Peptide, and Altered Key Molecular Pathways in the Pathogenesis and Progression of Alzheimer’s Disease

(2018) D. Allan Butterfield et al.   JOURNAL OF ALZHEIMERS DISEASE

Oxidative stress and the amyloid beta peptide in Alzheimer’s disease

(2018) C. Cheignon et al.   Redox Biology

BACE1 as a Potential Biomarker for Alzheimer's Disease

(2018) Boris Decourt et al.   JOURNAL OF ALZHEIMERS DISEASE

Distribution of Pathology in Frontal Variant Alzheimer's Disease

(2018) Richard Blennerhassett et al.   JOURNAL OF ALZHEIMERS DISEASE

Activated charcoal significantly improved the reliability of methods for quantitative analysis of endogenous substances in biological specimens: Glutathione and cysteine as cases

(2018) Boyu Shen et al.   JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES

Aberration of Nrf2‑Bach1 pathway in colorectal carcinoma; role in carcinogenesis and tumor progression

(2018) Heba E.M. El-Deek et al.   Annals of Diagnostic Pathology

Small molecules inhibiting Keap1–Nrf2 protein–protein interactions: a novel approach to activate Nrf2 function

(2017) Chunlin Zhuang et al.   MedChemComm

Direct Keap1-Nrf2 disruption as a potential therapeutic target for Alzheimer’s disease

(2017) Fiona Kerr et al.   PLoS Genetics

Distinct inflammatory phenotypes of microglia and monocyte-derived macrophages in Alzheimer's disease models: effects of aging and amyloid pathology

(2016) Elodie Martin et al.   AGING CELL

Redox-based therapeutics in neurodegenerative disease

(2016) G J McBean et al.   BRITISH JOURNAL OF PHARMACOLOGY

The Cellular Phase of Alzheimer’s Disease

(2016) Bart De Strooper et al.   CELL

The amyloid hypothesis of Alzheimer's disease at 25 years

(2016) Dennis J Selkoe et al.   EMBO Molecular Medicine

Discovery and Development of Kelch-like ECH-Associated Protein 1. Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein–Protein Interaction Inhibitors: Achievements, Challenges, and Future Directions

(2016) Zheng-Yu Jiang et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Keap1-Nrf2-ARE Pathway As a Potential Preventive and Therapeutic Target: An Update

(2016) Meng-Chen Lu et al.   MEDICINAL RESEARCH REVIEWS

Small molecules, big targets: drug discovery faces the protein–protein interaction challenge

(2016) Duncan E. Scott et al.   NATURE REVIEWS DRUG DISCOVERY

BACE1 in the retina: a sensitive biomarker for monitoring early pathological changes in Alzheimer′s disease

(2016) Hui Wang et al.   Neural Regeneration Research

Nrf2—a therapeutic target for the treatment of neurodegenerative diseases

(2015) Delinda A. Johnson et al.   FREE RADICAL BIOLOGY AND MEDICINE

Updated Research and Applications of Small Molecule Inhibitors of Keap1-Nrf2 Protein-Protein Interaction: a Review

(2014) Chunlin Zhuang et al.   CURRENT MEDICINAL CHEMISTRY

Rapid Identification of Keap1–Nrf2 Small-Molecule Inhibitors through Structure-Based Virtual Screening and Hit-Based Substructure Search

(2014) Chunlin Zhuang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Nrf2 reduces levels of phosphorylated tau protein by inducing autophagy adaptor protein NDP52

(2014) Chulman Jo et al.   Nature Communications

Oxidative stress and mitochondrial dysfunction in Alzheimer's disease

(2013) Xinglong Wang et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

Keap Calm, and Carry on Covalently

(2013) Anthony J. Wilson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bardoxolone Methyl in Type 2 Diabetes and Stage 4 Chronic Kidney Disease

(2013) Dick de Zeeuw et al.   NEW ENGLAND JOURNAL OF MEDICINE

Attenuation ofβ-Amyloid-Induced Oxidative Cell Death by Sulforaphane via Activation of NF-E2-Related Factor 2

(2013) Chan Lee et al.   Oxidative Medicine and Cellular Longevity

Small Molecule Modulators of Keap1-Nrf2-ARE Pathway as Potential Preventive and Therapeutic Agents

(2012) Sadagopan Magesh et al.   MEDICINAL RESEARCH REVIEWS

Remarkable Potential of the α-Aminophosphonate/Phosphinate Structural Motif in Medicinal Chemistry

(2011) Artur Mucha et al.   JOURNAL OF MEDICINAL CHEMISTRY

Integration, scaling, space-group assignment and post-refinement

(2010) Wolfgang Kabsch   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

XDS

(2010) Wolfgang Kabsch   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Oxidative stress in Alzheimer disease

(2010) Alejandro Gella et al.   Cell Adhesion & Migration

Triterpenoid CDDO-methylamide improves memory and decreases amyloid plaques in a transgenic mouse model of Alzheimer’s disease

(2009) Magali Dumont et al.   JOURNAL OF NEUROCHEMISTRY

Bicyclol: A Novel Drug for Treating Chronic Viral Hepatitis B and C

(2009) Geng Liu   Medicinal Chemistry

Intrahippocampal injection of a lentiviral vector expressing Nrf2 improves spatial learning in a mouse model of Alzheimer's disease

(2009) K. Kanninen et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Prodrugs of Phosphates and Phosphonates

(2008) Scott J. Hecker et al.   JOURNAL OF MEDICINAL CHEMISTRY