Design, synthesis and evaluation of novel small molecules acting as Keap1-Nrf2 protein-protein interaction inhibitors

Importance of Binding Site Hydration and Flexibility Revealed When Optimizing a Macrocyclic Inhibitor of the Keap1–Nrf2 Protein–Protein Interaction

(2022) Fabio Begnini et al.   JOURNAL OF MEDICINAL CHEMISTRY

Phenyl Bis-Sulfonamide Keap1-Nrf2 Protein–Protein Interaction Inhibitors with an Alternative Binding Mode

(2022) Nikolaos Georgakopoulos et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-activity relationships of 1,4-bis(arylsulfonamido)-benzene or naphthalene-N,N′-diacetic acids with varying C2-substituents as inhibitors of Keap1-Nrf2 protein-protein interaction

(2022) Sumi Lee et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of disubstituted xylylene derivatives as small molecule direct inhibitors of Keap1-Nrf2 protein-protein interaction

(2020) Dhulfiqar Ali Abed et al.   BIOORGANIC & MEDICINAL CHEMISTRY

The Molecular Mechanisms Regulating the KEAP1-NRF2 Pathway

(2020) Liam Baird et al.   MOLECULAR AND CELLULAR BIOLOGY

Combined Peptide and Small-Molecule Approach toward Nonacidic THIQ Inhibitors of the KEAP1/NRF2 Interaction

(2020) Jesus M. Ontoria et al.   ACS Medicinal Chemistry Letters

Design, Synthesis, and Structure–Activity Relationships of Indoline-Based Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-Like 2 (Keap1-Nrf2) Protein–Protein Interaction Inhibitors

(2020) Hai-Shan Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Isoquinoline Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-like 2 (KEAP1-NRF2) Inhibitors with High Metabolic Stability

(2019) Phillip R. Lazzara et al.   JOURNAL OF MEDICINAL CHEMISTRY

Dimethyl fumarate attenuates lipopolysaccharide-induced mitochondrial injury by activating Nrf2 pathway in cardiomyocytes

(2019) Chun-Yan Fu et al.   LIFE SCIENCES

ROS and diseases: role in metabolism and energy supply

(2019) Shenshu Yang et al.   MOLECULAR AND CELLULAR BIOCHEMISTRY

Oxidative Stress and Cancer: The Role of Nrf2

(2018) Soraya Sajadimajd et al.   CURRENT CANCER DRUG TARGETS

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

The KEAP1-NRF2 System: a Thiol-Based Sensor-Effector Apparatus for Maintaining Redox Homeostasis

(2018) Masayuki Yamamoto et al.   PHYSIOLOGICAL REVIEWS

Serum amyloid A promotes LPS clearance and suppresses LPS‐induced inflammation and tissue injury

(2018) Ni Cheng et al.   EMBO REPORTS

SwissADME: a free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules

(2017) Antoine Daina et al.   Scientific Reports

Transcriptional Regulation by Nrf2

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

Sepsis: in search of cure

(2016) Chikkamenahalli Lakshminarayana Lakshmikanth et al.   INFLAMMATION RESEARCH

Sulforaphane and Other Nutrigenomic Nrf2 Activators: Can the Clinician’s Expectation Be Matched by the Reality?

(2016) Christine A. Houghton et al.   Oxidative Medicine and Cellular Longevity

Mutagenicity in a Molecule: Identification of Core Structural Features of Mutagenicity Using a Scaffold Analysis

(2016) Kuo-Hsiang Hsu et al.   PLoS One

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

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

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

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

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

(2012) Sadagopan Magesh et al.   MEDICINAL RESEARCH REVIEWS

Chemistry and biology of reactive oxygen species in signaling or stress responses

(2011) Bryan C Dickinson et al.   Nature Chemical Biology

Small molecule modulators of antioxidant response pathway

(2010) Wooyoung Hur et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

New Substructure Filters for Removal of Pan Assay Interference Compounds (PAINS) from Screening Libraries and for Their Exclusion in Bioassays

(2010) Jonathan B. Baell et al.   JOURNAL OF MEDICINAL CHEMISTRY