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

Filtering promiscuous compounds in early drug discovery: is it a good idea?

(2016) Mario R. Senger et al.   DRUG DISCOVERY TODAY

Redox signaling: An evolution from free radicals to aging

(2016) Henry Jay Forman   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

Design, Synthesis, and Initial Evaluation of Affinity-Based Small-Molecule Probes for Fluorescent Visualization and Specific Detection of Keap1

(2016) Mengchen Lu et al.   JOURNAL OF 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

Discovery of a Selective Aurora A Kinase Inhibitor by Virtual Screening

(2016) Falco Kilchmann 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

A systematic molecular dynamics approach to the study of peptide Keap1–Nrf2 protein–protein interaction inhibitors and its application to p62 peptides

(2016) Meng-Chen Lu et al.   Molecular BioSystems

Polar Recognition Group Study of Keap1-Nrf2 Protein–Protein Interaction Inhibitors

(2016) Meng-Chen Lu et al.   ACS Medicinal Chemistry Letters

p62/Sqstm1 promotes malignancy of HCV-positive hepatocellular carcinoma through Nrf2-dependent metabolic reprogramming

(2016) Tetsuya Saito et al.   Nature Communications

Exercise, Nrf2 and Antioxidant Signaling in Cardiac Aging

(2016) Madhusudhanan Narasimhan et al.   Frontiers in Physiology

The Keap1/Nrf2 pathway in health and disease: from the bench to the clinic

(2015) Maria A. O’Connell et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

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

(2015) Chunquan Sheng et al.   CHEMICAL SOCIETY REVIEWS

Probing the structural requirements of non-electrophilic naphthalene-based Nrf2 activators

(2015) Atul D. Jain et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Molecular basis of the Keap1–Nrf2 system

(2015) Takafumi Suzuki et al.   FREE RADICAL BIOLOGY AND MEDICINE

Nrf2—a therapeutic target for the treatment of neurodegenerative diseases

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

Characterization of RA839, a Noncovalent Small Molecule Binder to Keap1 and Selective Activator of Nrf2 Signaling

(2015) Angelika F. Winkel et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

Mitigating risk in academic preclinical drug discovery

(2015) Jayme L. Dahlin et al.   NATURE REVIEWS DRUG DISCOVERY

The emerging role of redox-sensitive Nrf2–Keap1 pathway in diabetes

(2015) Elango Bhakkiyalakshmi et al.   PHARMACOLOGICAL RESEARCH

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

Modulation of NRF2 signaling pathway by nuclear receptors: Implications for cancer

(2014) Akhileshwar Namani et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Binding Mode and Structure-Activity Relationships around Direct Inhibitors of the Nrf2-Keap1 Complex

(2014) Eric Jnoff et al.   ChemMedChem

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

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

Drug-Like ProteinProtein Interaction Modulators: Challenges and Opportunities for Drug Discovery and Chemical Biology

(2014) Bruno O. Villoutreix et al.   Molecular Informatics

Chemistry: Chemical con artists foil drug discovery

(2014) Jonathan Baell et al.   NATURE

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

Discovery of a small-molecule inhibitor and cellular probe of Keap1–Nrf2 protein–protein interaction

(2013) Longqin Hu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2013) H. Wang et al.   CANCER RESEARCH

Oxidative stress in carcinogenesis: new synthetic compounds with dual effects upon free radicals and cancer.

(2013) Betul Tekiner-Gulbas et al.   CURRENT MEDICINAL CHEMISTRY

Keap Calm, and Carry on Covalently

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

NRF2-regulation in brain health and disease: Implication of cerebral inflammation

(2013) Mats Sandberg et al.   NEUROPHARMACOLOGY

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

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

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

(2013) Hao-Peng Sun et al.   MedChemComm

Structure-Based Virtual Screening for Drug Discovery: a Problem-Centric Review

(2012) Tiejun Cheng et al.   AAPS Journal

Gene Therapy Targeting Inflammation in Atherosclerosis

(2012) Tim Van-Assche et al.   CURRENT PHARMACEUTICAL DESIGN

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

(2012) Sadagopan Magesh et al.   MEDICINAL RESEARCH REVIEWS

Nrf2 is controlled by two distinct β-TrCP recognition motifs in its Neh6 domain, one of which can be modulated by GSK-3 activity

(2012) S Chowdhry et al.   ONCOGENE

Structural biology and drug discovery for protein–protein interactions

(2012) Harry Jubb et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

State-of-the-art in ligand-based virtual screening

(2011) Peter Ripphausen et al.   DRUG DISCOVERY TODAY

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

Redox signaling in inflammation: interactions of endogenous electrophiles and mitochondria in cardiovascular disease

(2010) Jeffrey R. Koenitzer et al.   Annals of the New York Academy of Sciences

Cancer Chemoprevention Mechanisms Mediated Through the Keap1–Nrf2 Pathway

(2010) John D. Hayes et al.   ANTIOXIDANTS & REDOX SIGNALING

Discovery of the Negative Regulator of Nrf2, Keap1: A Historical Overview

(2010) Ken Itoh et al.   ANTIOXIDANTS & REDOX SIGNALING

Oxidative stress, inflammation, and cancer: How are they linked?

(2010) Simone Reuter et al.   FREE RADICAL BIOLOGY AND MEDICINE

Targeting NRF2 signaling for cancer chemoprevention

(2009) Mi-Kyoung Kwak et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Physiological Significance of Reactive Cysteine Residues of Keap1 in Determining Nrf2 Activity

(2008) T. Yamamoto et al.   MOLECULAR AND CELLULAR BIOLOGY

Molecular mechanisms of Nrf2-mediated antioxidant response

(2008) Wenge Li et al.   MOLECULAR CARCINOGENESIS