Emerging Screening Approaches in the Development of Nrf2–Keap1 Protein–Protein Interaction Inhibitors

Pharmacological Applications of Nrf2 Inhibitors as Potential Antineoplastic Drugs

(2019) Pelin Telkoparan-Akillilar et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Structure–Activity and Structure–Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein–Protein Interaction

(2019) Tom D. Heightman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Potential Applications of NRF2 Inhibitors in Cancer Therapy

(2019) Emiliano Panieri et al.   Oxidative Medicine and Cellular Longevity

Discovery of a Potent Kelch-Like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1–Nrf2) Protein–Protein Interaction Inhibitor with Natural Proline Structure as a Cytoprotective Agent against Acetaminophen-Induced Hepatotoxicity

(2019) Meng-Chen Lu et al.   JOURNAL OF MEDICINAL CHEMISTRY

CPUY192018, a potent inhibitor of the Keap1-Nrf2 protein-protein interaction, alleviates renal inflammation in mice by restricting oxidative stress and NF-κB activation

(2019) Meng-Chen Lu et al.   Redox Biology

Design, synthesis, and evaluation of NDGA analogues as potential anti-ischemic stroke agents

(2018) Lili Huang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Activation of anti-oxidant Nrf2 signaling by enone analogues of curcumin

(2018) Lorraine M. Deck et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a head-to-tail cyclic peptide as the Keap1-Nrf2 protein-protein interaction inhibitor with high cell potency

(2018) Meng-Chen Lu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

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

Identification of a novel small-molecule Keap1–Nrf2 PPI inhibitor with cytoprotective effects on LPS-induced cardiomyopathy

(2018) Cheng-Shi Jiang et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Triptolide enhances chemotherapeutic efficacy of antitumor drugs in non-small-cell lung cancer cells by inhibiting Nrf2-ARE activity

(2018) Jiayu Zhu et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Drug screening assay based on the interaction of intact Keap1 and Nrf2 proteins in cancer cells

(2018) Bo Zhou et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Deep learning and virtual drug screening

(2018) Kristy A Carpenter et al.   Future Medicinal Chemistry

Pharmacological Inhibition of LSD1 for Cancer Treatment

(2018) Guan-Jun Yang et al.   MOLECULES

Schisandrin B elicits the Keap1-Nrf2 defense system via carbene reactive metabolite which is less harmful to mice liver

(2018) Shan Feng et al.   Drug Design Development and Therapy

GPU Accelerated Quantum Virtual Screening: Application for the Natural Inhibitors of New Dehli Metalloprotein (NDM-1)

(2018) Mingsong Shi et al.   Frontiers in Chemistry

Development of a High-Throughput Cul3-Keap1 Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) Assay for Identifying Nrf2 Activators

(2018) Derek D. Poore et al.   SLAS Discovery

Ellagic acid ameliorates oxidative stress and insulin resistance in high glucose-treated HepG2 cells via miR-223/keap1-Nrf2 pathway

(2018) Xiaoqin Ding et al.   BIOMEDICINE & PHARMACOTHERAPY

Halofuginone enhances the chemo-sensitivity of cancer cells by suppressing NRF2 accumulation

(2017) Kouhei Tsuchida et al.   FREE RADICAL BIOLOGY AND MEDICINE

Fragment-based virtual screening approach and molecular dynamics simulation studies for identification of BACE1 inhibitor leads

(2017) Prabu Manoharan et al.   JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS

KEAP1-modifying small molecule reveals muted NRF2 signaling responses in neural stem cells from Huntington's disease patients

(2017) Luisa Quinti et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2017) Chunlin Zhuang et al.   MedChemComm

Clinical Neurology and Epidemiology of the Major Neurodegenerative Diseases

(2017) Michael G. Erkkinen et al.   Cold Spring Harbor Perspectives in Biology

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

(2017) Fiona Kerr et al.   PLoS Genetics

Drug-Repositioning Screening for Keap1-Nrf2 Binding Inhibitors using Fluorescence Correlation Spectroscopy

(2017) Yuki Yoshizaki et al.   Scientific Reports

Transcriptional Regulation by Nrf2

(2017) Claudia Tonelli et al.   ANTIOXIDANTS & REDOX SIGNALING

Small Molecule Inhibitor of NRF2 Selectively Intervenes Therapeutic Resistance in KEAP1-Deficient NSCLC Tumors

(2016) Anju Singh et al.   ACS Chemical Biology

Identification of an adaptor protein that facilitates Nrf2-Keap1 complex formation and modulates antioxidant response

(2016) Yuxue Zhang et al.   FREE RADICAL BIOLOGY AND MEDICINE

Synthesis and biological evaluation of novel 2-phenylquinazoline-4-amine derivatives: identification of 6-phenyl-8H-benzo[g]quinazolino[4,3-b]quinazolin-8-one as a highly potent inducer of NAD(P)H quinone oxidoreductase 1

(2016) Mostafa M. Ghorab et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein–Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery

(2016) Thomas G. Davies 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

NRF2, a Key Regulator of Antioxidants with Two Faces towards Cancer

(2016) Jaieun Kim et al.   Oxidative Medicine and Cellular Longevity

Open challenges in structure-based virtual screening: Receptor modeling, target flexibility consideration and active site water molecules description

(2015) Francesca Spyrakis et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Peptide and small molecule inhibitors of the Keap1–Nrf2 protein–protein interaction

(2015) Geoff Wells   BIOCHEMICAL SOCIETY TRANSACTIONS

Role of growth hormone in maturation and activation of dendritic cellsviamiR-200a and the Keap1/Nrf2 pathway

(2015) Qiu-Liang Liu et al.   CELL PROLIFERATION

State-of-the-art strategies for targeting protein–protein interactions by small-molecule inhibitors

(2015) Chunquan Sheng et al.   CHEMICAL SOCIETY REVIEWS

Functional polymorphisms in Nrf2 : implications for human disease

(2015) Hye-Youn Cho et al.   FREE RADICAL BIOLOGY AND MEDICINE

Structure–Activity and Structure–Property Relationship and Exploratory in Vivo Evaluation of the Nanomolar Keap1–Nrf2 Protein–Protein Interaction Inhibitor

(2015) Zheng-Yu Jiang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Evaluation of Triazole Derivatives That Induce Nrf2 Dependent Gene Products and Inhibit the Keap1–Nrf2 Protein–Protein Interaction

(2015) Hélène C. Bertrand et al.   JOURNAL OF MEDICINAL CHEMISTRY

Oxidative Stress in Neurodegenerative Diseases

(2015) Ewa Niedzielska et al.   MOLECULAR NEUROBIOLOGY

MUC1-C activates the TAK1 inflammatory pathway in colon cancer

(2015) H Takahashi et al.   ONCOGENE

Dipeptidyl peptidase-4 inhibition by gemigliptin prevents abnormal vascular remodeling via NF-E2-related factor 2 activation

(2015) Seung Hee Choi et al.   VASCULAR PHARMACOLOGY

Expression of xCT and activity of system x c − are regulated by NRF2 in human breast cancer cells in response to oxidative stress

(2015) Eric Habib et al.   Redox Biology

Discovery of direct inhibitors of Keap1–Nrf2 protein–protein interaction as potential therapeutic and preventive agents

(2015) Dhulfiqar Ali Abed et al.   Acta Pharmaceutica Sinica B

Nrf2 and Redox Status in Prediabetic and Diabetic Patients

(2014) Angélica Jiménez-Osorio et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

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

Discovery of Potent Keap1–Nrf2 Protein–Protein Interaction Inhibitor Based on Molecular Binding Determinants Analysis

(2014) Zheng-Yu Jiang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small molecules inhibit the interaction of Nrf2 and the Keap1 Kelch domain through a non-covalent mechanism

(2013) Douglas Marcotte et al.   BIOORGANIC & MEDICINAL CHEMISTRY

RXR  Inhibits the NRF2-ARE Signaling Pathway through a Direct Interaction with the Neh7 Domain of NRF2

(2013) H. Wang et al.   CANCER RESEARCH

Phosphorylation of p62 Activates the Keap1-Nrf2 Pathway during Selective Autophagy

(2013) Yoshinobu Ichimura et al.   MOLECULAR CELL

Peptide inhibitors of the Keap1–Nrf2 protein–protein interaction with improved binding and cellular activity

(2013) Rowena Hancock et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Development of a steady-state FRET-based assay to identify inhibitors of the Keap1-Nrf2 protein-protein interaction

(2013) Marjolein Schaap et al.   PROTEIN SCIENCE

Novel protein–protein interaction inhibitor of Nrf2–Keap1 discovered by structure-based virtual screening

(2013) Hao-Peng Sun et al.   MedChemComm

The Keap1-Nrf2 pathway: Mechanisms of activation and dysregulation in cancer

(2013) Emilia Kansanen et al.   Redox Biology

Nuclear Factor Erythroid 2-Related Factor 2 Nuclear Translocation Induces Myofibroblastic Dedifferentiation in Idiopathic Pulmonary Fibrosis

(2012) Elise Artaud-Macari et al.   ANTIOXIDANTS & REDOX SIGNALING

Nrf2–keap1 system versus NF-κB: The good and the evil in chronic kidney disease?

(2012) Liliana Magnago Pedruzzi et al.   BIOCHIMIE

Keap1: One stone kills three birds Nrf2, IKKβ and Bcl-2/Bcl-xL

(2012) Hui Tian et al.   CANCER LETTERS

Ellagic acid protects human keratinocyte (HaCaT) cells against UVA-induced oxidative stress and apoptosis through the upregulation of the HO-1 and Nrf-2 antioxidant genes

(2012) You-Cheng Hseu et al.   FOOD AND CHEMICAL TOXICOLOGY

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

(2012) Sadagopan Magesh et al.   MEDICINAL RESEARCH REVIEWS

Emerging roles of Nrf2 and phase II antioxidant enzymes in neuroprotection

(2012) Meijuan Zhang et al.   PROGRESS IN NEUROBIOLOGY

Dietary modulation of the biotransformation and genotoxicity of aflatoxin B1

(2012) Kerstin Gross-Steinmeyer et al.   TOXICOLOGY

Development of Neh2-Luciferase Reporter and Its Application for High Throughput Screening and Real-Time Monitoring of Nrf2 Activators

(2011) Natalya A. Smirnova et al.   CHEMISTRY & BIOLOGY

Peptide inhibitors of the Keap1–Nrf2 protein–protein interaction

(2011) Rowena Hancock et al.   FREE RADICAL BIOLOGY AND MEDICINE

Druggability assessment of protein–protein interfaces

(2011) Jutta Wanner et al.   Future Medicinal Chemistry

Molecular mechanisms of the Keap1-Nrf2 pathway in stress response and cancer evolution

(2011) Keiko Taguchi et al.   GENES TO CELLS

Bardoxolone Methyl and Kidney Function in CKD with Type 2 Diabetes

(2011) Pablo E. Pergola et al.   NEW ENGLAND JOURNAL OF MEDICINE

NRF2 targeting: a promising therapeutic strategy in chronic obstructive pulmonary disease

(2011) A. Boutten et al.   TRENDS IN MOLECULAR MEDICINE

Nrf2: friend or foe for chemoprevention?

(2009) T. W. Kensler et al.   CARCINOGENESIS

Hydrogen Peroxide Is a Second Messenger in Phase 2 Enzyme Induction by Cancer Chemopreventive Dithiolethiones

(2009) Ryan Holland et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Targeting the Nrf2 pathway against cardiovascular disease

(2009) Jinqing Li et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Hyperglycemia induces oxidative and nitrosative stress and increases renal functional impairment in Nrf2-deficient mice

(2008) Keigyou Yoh et al.   GENES TO CELLS

Molecular mechanisms of Nrf2-mediated antioxidant response

(2008) Wenge Li et al.   MOLECULAR CARCINOGENESIS

Functional organization of the basal ganglia: Therapeutic implications for Parkinson's disease

(2008) Jose A. Obeso et al.   MOVEMENT DISORDERS

Dual roles of Nrf2 in cancer

(2008) A LAU et al.   PHARMACOLOGICAL RESEARCH