Methyl and Fluorine Effects in Novel Orally Bioavailable Keap1–Nrf2 PPI Inhibitor

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

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

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

Insight into Thermodynamic and Kinetic Profiles in Small-Molecule Optimization

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

KEAP1‐NRF2 protein–protein interaction inhibitors: Design, pharmacological properties and therapeutic potential

(2022) Enrique Crisman et al.   MEDICINAL RESEARCH REVIEWS

Development of Noncovalent Small-Molecule Keap1-Nrf2 Inhibitors by Fragment-Based Drug Discovery

(2022) Dilip Narayanan et al.   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

A hydrogen peroxide responsive prodrug of Keap1-Nrf2 inhibitor for improving oral absorption and selective activation in inflammatory conditions

(2020) Mengchen Lu et al.   Redox Biology

Recent progress in Keap1-Nrf2 protein-protein interaction inhibitors

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

Dapagliflozin in Patients with Chronic Kidney Disease

(2020) Hiddo J.L. Heerspink et al.   NEW ENGLAND JOURNAL OF MEDICINE

Effect of Finerenone on Chronic Kidney Disease Outcomes in Type 2 Diabetes

(2020) George L. Bakris et al.   NEW ENGLAND JOURNAL OF MEDICINE

Canagliflozin and Renal Outcomes in Type 2 Diabetes and Nephropathy

(2019) Vlado Perkovic et al.   NEW ENGLAND JOURNAL OF MEDICINE

A single number for advocacy and communication—worldwide more than 850 million individuals have kidney diseases

(2019) Kitty J. Jager et al.   KIDNEY INTERNATIONAL

Design, synthesis and identification of novel, orally bioavailable non-covalent Nrf2 activators

(2019) Bin Ma et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Replacement of a Naphthalene Scaffold in Kelch-like ECH-Associated Protein 1 (KEAP1)/Nuclear Factor (Erythroid-derived 2)-like 2 (NRF2) Inhibitors

(2018) Benjamin G. Richardson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Forecasting life expectancy, years of life lost, and all-cause and cause-specific mortality for 250 causes of death: reference and alternative scenarios for 2016–40 for 195 countries and territories

(2018) Kyle J Foreman et al.   LANCET

Thermodynamic profiling of inhibitors of Nrf2:Keap1 interactions

(2016) Hamid R. Nasiri et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

Applying thermodynamic profiling in lead finding and optimization

(2015) Gerhard Klebe   NATURE REVIEWS DRUG DISCOVERY

Mechanisms Contributing to Adverse Cardiovascular Events in Patients with Type 2 Diabetes Mellitus and Stage 4 Chronic Kidney Disease Treated with Bardoxolone Methyl

(2014) Melanie P. Chin et al.   AMERICAN JOURNAL OF NEPHROLOGY

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

(2014) Eric Jnoff et al.   ChemMedChem

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

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

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

Bardoxolone Methyl and Kidney Function in CKD with Type 2 Diabetes

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

Synthesis and Vanilloid Receptor (TRPV1) Activity of the Enantiomers of α-Fluorinated Capsaicin

(2009) Margit Winkler et al.   CHEMBIOCHEM

The Many Roles for Fluorine in Medicinal Chemistry

(2008) William K. Hagmann   JOURNAL OF MEDICINAL CHEMISTRY

Role of the Active-Site Solvent in the Thermodynamics of Factor Xa Ligand Binding

(2008) Robert Abel et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY