Harnessing the E3 Ligase KEAP1 for Targeted Protein Degradation

Nrf2 activation through the inhibition of Keap1–Nrf2 protein–protein interaction

(2020) Sumi Lee et al.   MEDICINAL CHEMISTRY RESEARCH

Opposing Functions of BRD4 Isoforms in Breast Cancer

(2020) Shwu-Yuan Wu et al.   MOLECULAR CELL

Roles of the BRD4 short isoform in phase separation and active gene transcription

(2020) Xinye Han et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

CDDO-Imidazolide Targets Multiple Amino Acid Residues on the Nrf2 Adaptor, Keap1

(2020) Xiaoli Meng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bardoxolone conjugation enables targeted protein degradation of BRD4

(2020) Bingqi Tong et al.   Scientific Reports

Structure–Activity and Structure–Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein–Protein Interaction

(2019) Tom D. Heightman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeted protein degradation: expanding the toolbox

(2019) Matthieu Schapira et al.   NATURE REVIEWS DRUG DISCOVERY

Discovery of a first-in-class EZH2 selective degrader

(2019) Anqi Ma et al.   Nature Chemical Biology

Discovery of a Keap1-dependent peptide PROTAC to knockdown Tau by ubiquitination-proteasome degradation pathway

(2018) Mengchen Lu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Non-covalent Small-Molecule Kelch-like ECH-Associated Protein 1–Nuclear Factor Erythroid 2-Related Factor 2 (Keap1–Nrf2) Inhibitors and Their Potential for Targeting Central Nervous System Diseases

(2018) Jakob S. Pallesen et al.   JOURNAL OF MEDICINAL CHEMISTRY

MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53

(2018) John Hines et al.   CANCER RESEARCH

BRD4 and Cancer: going beyond transcriptional regulation

(2018) Benedetta Donati et al.   Molecular Cancer

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

Catalytic in vivo protein knockdown by small-molecule PROTACs

(2015) Daniel P Bondeson et al.   Nature Chemical Biology

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

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

(2014) Anne Cleasby et al.   PLoS One

The emerging family of CULLIN3-RING ubiquitin ligases (CRL3s): cellular functions and disease implications

(2013) Pascal Genschik et al.   EMBO JOURNAL

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

(2011) Jake E. Delmore et al.   CELL

Proteomic Analysis Shows Synthetic Oleanane Triterpenoid Binds to mTOR

(2011) Mark M. Yore et al.   PLoS One

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE