Screening approaches for the identification of Nrf2-Keap1 protein-protein interaction inhibitors targeting hot spot residues

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

(2023) Kazuki Otake et al.   ACS Medicinal Chemistry Letters

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

(2022) Enrique Crisman et al.   MEDICINAL RESEARCH REVIEWS

Therapeutic Targeting of the NRF2 Signaling Pathway in Cancer

(2021) Pelin Telkoparan-Akillilar et al.   MOLECULES

Artificial intelligence based methods for hot spot prediction

(2021) Damla Ovek et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Applied Biophysical Methods in Fragment-Based Drug Discovery

(2020) Joe Coyle et al.   SLAS Discovery

Interaction Energetics and Druggability of the Protein–Protein Interaction between Kelch-like ECH-Associated Protein 1 (KEAP1) and Nuclear Factor Erythroid 2 Like 2 (Nrf2)

(2019) Mengqi Zhong et al.   BIOCHEMISTRY

Application of Native ESI-MS to Characterize Interactions between Compounds Derived from Fragment-Based Discovery Campaigns and Two Pharmaceutically Relevant Proteins

(2018) Agni F. M. Gavriilidou et al.   SLAS Discovery

High-Throughput Screening for Linear Ubiquitin Chain Assembly Complex (LUBAC) Selective Inhibitors Using Homogenous Time-Resolved Fluorescence (HTRF)-Based Assay System

(2018) Ken Katsuya et al.   SLAS Discovery

Biophysics: for HTS hit validation, chemical lead optimization, and beyond

(2017) Christine C. Genick et al.   Expert Opinion on Drug Discovery

Enthalpy screen of drug candidates

(2016) Arne Schön et al.   ANALYTICAL BIOCHEMISTRY

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

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

Structural basis of Keap1 interactions with Nrf2

(2015) Peter Canning et al.   FREE RADICAL BIOLOGY AND MEDICINE

Hot spot-based design of small-molecule inhibitors for protein–protein interactions

(2014) Wenxing Guo et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Small-Molecule Inhibitors of Protein-Protein Interactions: Progressing toward the Reality

(2014) Michelle R. Arkin et al.   CHEMISTRY & BIOLOGY

Comparison of the sensitivities of WaterLOGSY and saturation transfer difference NMR experiments

(2014) Aleksandar Antanasijevic et al.   JOURNAL OF BIOMOLECULAR NMR

Label Free Fragment Screening Using Surface Plasmon Resonance as a Tool for Fragment Finding – Analyzing Parkin, a Difficult CNS Target

(2013) Karin Regnström et al.   PLoS One

Development of an efficient E. coli expression and purification system for a catalytically active, human Cullin3–RINGBox1 protein complex and elucidation of its quaternary structure with Keap1

(2010) Evan Small et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Nrf2:INrf2 (Keap1) signaling in oxidative stress

(2009) James W. Kaspar et al.   FREE RADICAL BIOLOGY AND MEDICINE

Do enthalpy and entropy distinguish first in class from best in class?

(2008) E FREIRE   DRUG DISCOVERY TODAY

Surface Plasmon Resonance Based Assay for the Detection and Characterization of Promiscuous Inhibitors

(2008) Anthony M. Giannetti et al.   JOURNAL OF MEDICINAL CHEMISTRY

Assembly reflects evolution of protein complexes

(2008) Emmanuel D. Levy et al.   NATURE

Isothermal titration calorimetry at very low c

(2007) Joel Tellinghuisen   ANALYTICAL BIOCHEMISTRY