Design and characterization of a heterobifunctional degrader of KEAP1

Optimization of Phosphotyrosine Peptides that Target the SH2 Domain of SOCS1 and Block Substrate Ubiquitination

(2022) Hao Chen et al.   ACS Chemical Biology

Deconstructing Noncovalent Kelch-like ECH-Associated Protein 1 (Keap1) Inhibitors into Fragments to Reconstruct New Potent Compounds

(2021) Jakob S. Pallesen et al.   JOURNAL OF MEDICINAL CHEMISTRY

From Conception to Development: Investigating PROTACs Features for Improved Cell Permeability and Successful Protein Degradation

(2021) Carlotta Cecchini et al.   Frontiers in Chemistry

Harnessing the E3 Ligase KEAP1 for Targeted Protein Degradation

(2021) Jieli Wei et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Phenyl‐Glutarimides: Alternative Cereblon Binders for the Design of PROTACs

(2021) Jaeki Min et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Influence of Linker Attachment Points on the Stability and Neosubstrate Degradation of Cereblon Ligands

(2021) Aleša Bricelj et al.   ACS Medicinal Chemistry Letters

Proteolysis‐targeting chimeras in drug development: A safety perspective

(2020) Kevin Moreau et al.   BRITISH JOURNAL OF PHARMACOLOGY

Recent progress in the development of small molecule Nrf2 activators: a patent review (2017-present)

(2020) Haishan Zhou et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

The Molecular Mechanisms Regulating the KEAP1-NRF2 Pathway

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

NRF2, a Transcription Factor for Stress Response and Beyond

(2020) Feng He et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Systematic Investigation of the Permeability of Androgen Receptor PROTACs

(2020) Duncan E. Scott et al.   ACS Medicinal Chemistry Letters

KEAP1, a cysteine-based sensor and a drug target for the prevention and treatment of chronic disease

(2020) Sharadha Dayalan Naidu et al.   Open Biology

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

Iron Metabolism in Ferroptosis

(2020) Xin Chen et al.   Frontiers in Cell and Developmental Biology

The PROTAC technology in drug development

(2019) Yutian Zou et al.   CELL BIOCHEMISTRY AND FUNCTION

Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer

(2019) Xin Han et al.   JOURNAL OF MEDICINAL CHEMISTRY

Therapeutic targeting of the NRF2 and KEAP1 partnership in chronic diseases

(2019) Antonio Cuadrado et al.   NATURE REVIEWS DRUG DISCOVERY

Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs

(2019) Miriam Girardini et al.   BIOORGANIC & MEDICINAL CHEMISTRY

BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design

(2019) William Farnaby et al.   Nature Chemical Biology

Assessing the Cell Permeability of Bivalent Chemical Degraders Using the Chloroalkane Penetration Assay

(2019) Caroline A. Foley et al.   ACS Chemical Biology

Disordered region of cereblon is required for efficient degradation by proteolysis-targeting chimera

(2019) Kidae Kim et al.   Scientific Reports

Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression

(2018) Yangbing Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

Oxidative Stress: Harms and Benefits for Human Health

(2017) Gabriele Pizzino et al.   Oxidative Medicine and Cellular Longevity

pSILAC mass spectrometry reveals ZFP91 as IMiD-dependent substrate of the CRL4CRBN ubiquitin ligase

(2017) Jian An et al.   Nature Communications

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

Induced protein degradation: an emerging drug discovery paradigm

(2016) Ashton C. Lai et al.   NATURE REVIEWS DRUG DISCOVERY

Structural basis of Keap1 interactions with Nrf2

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

Oxidative stress: a concept in redox biology and medicine

(2015) Helmut Sies   Redox Biology

Structure of the BTB Domain of Keap1 and Its Interaction with the Triterpenoid Antagonist CDDO

(2014) Anne Cleasby et al.   PLoS One

Structural Basis for Cul3 Protein Assembly with the BTB-Kelch Family of E3 Ubiquitin Ligases

(2013) Peter Canning et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The selective autophagy substrate p62 activates the stress responsive transcription factor Nrf2 through inactivation of Keap1

(2010) Masaaki Komatsu et al.   NATURE CELL BIOLOGY