C151 in KEAP1 is the main cysteine sensor for the cyanoenone class of NRF2 activators, irrespective of molecular size or shape

KEAP1 inhibition is neuroprotective and suppresses the development of epilepsy

(2018) Tawfeeq Shekh-Ahmad et al.   BRAIN

Itaconate is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1

(2018) Evanna L. Mills et al.   NATURE

Activation of Nrf2 Signaling Augments Vesicular Stomatitis Virus Oncolysis via Autophagy-Driven Suppression of Antiviral Immunity

(2017) David Olagnier et al.   MOLECULAR THERAPY

In Situ Observation of Thiol Michael Addition to a Reversible Covalent Drug in a Crystalline Sponge

(2016) Vincent Duplan et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Characterization of novel small-molecule NRF2 activators: Structural and biochemical validation of stereospecific KEAP1 binding

(2016) Carlos Huerta et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

The acetylenic tricyclic bis(cyano enone), TBE-31, targets microtubule dynamics and cell polarity in migrating cells

(2016) Eddie Chan et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Electron affinity of tricyclic, bicyclic, and monocyclic compounds containing cyanoenones correlates with their potency as inducers of a cytoprotective enzyme

(2016) René V. Bensasson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Antidepressant effects of TBE-31 and MCE-1, the novel Nrf2 activators, in an inflammation model of depression

(2016) Wei Yao et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Nrf2 suppresses macrophage inflammatory response by blocking proinflammatory cytokine transcription

(2016) Eri H. Kobayashi et al.   Nature Communications

Loss of Nrf2 abrogates the protective effect of Keap1 downregulation in a preclinical model of cutaneous squamous cell carcinoma

(2016) Elena V. Knatko et al.   Scientific Reports

Pharmacokinetics and pharmacodynamics of orally administered acetylenic tricyclic bis (cyanoenone), a highly potent Nrf2 activator with a reversible covalent mode of action

(2015) Rumen V. Kostov et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Nrf2 Activation Protects against Solar-Simulated Ultraviolet Radiation in Mice and Humans

(2015) E. V. Knatko et al.   Cancer Prevention Research

New Monocyclic, Bicyclic, and Tricyclic Ethynylcyanodienones as Activators of the Keap1/Nrf2/ARE Pathway and Inhibitors of Inducible Nitric Oxide Synthase

(2015) Wei Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

Characterizations of Three Major Cysteine Sensors of Keap1 in Stress Response

(2015) Ryota Saito et al.   MOLECULAR AND CELLULAR BIOLOGY

Whole-BodyIn VivoMonitoring of Inflammatory Diseases Exploiting Human Interleukin 6-Luciferase Transgenic Mice

(2015) Makiko Hayashi et al.   MOLECULAR AND CELLULAR BIOLOGY

The PTEN/NRF2 Axis Promotes Human Carcinogenesis

(2014) Ana I. Rojo et al.   ANTIOXIDANTS & REDOX SIGNALING

Transcription Factors NRF2 and NF-κB Are Coordinated Effectors of the Rho Family, GTP-binding Protein RAC1 during Inflammation

(2014) Antonio Cuadrado et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

(2014) Anne Cleasby et al.   PLoS One

The Nrf2 regulatory network provides an interface between redox and intermediary metabolism

(2014) John D. Hayes et al.   TRENDS IN BIOCHEMICAL SCIENCES

Toward clinical application of the Keap1–Nrf2 pathway

(2013) Takafumi Suzuki et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Validation of the multiple sensor mechanism of the Keap1-Nrf2 system

(2012) Kai Takaya et al.   FREE RADICAL BIOLOGY AND MEDICINE

Synthesis, Chemical Reactivity as Michael Acceptors, and Biological Potency of Monocyclic Cyanoenones, Novel and Highly Potent Anti-inflammatory and Cytoprotective Agents

(2012) Suqing Zheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural and Functional Characterization of Nrf2 Degradation by the Glycogen Synthase Kinase 3/ -TrCP Axis

(2012) P. Rada et al.   MOLECULAR AND CELLULAR BIOLOGY

Nrf2 is controlled by two distinct β-TrCP recognition motifs in its Neh6 domain, one of which can be modulated by GSK-3 activity

(2012) S Chowdhry et al.   ONCOGENE

Guggulsterone induces heme oxygenase-1 expression through activation of Nrf2 in human mammary epithelial cells: PTEN as a putative target

(2011) I. Almazari et al.   CARCINOGENESIS

Tricyclic Compounds Containing Nonenolizable Cyano Enones. A Novel Class of Highly Potent Anti-Inflammatory and Cytoprotective Agents(79)

(2011) Tadashi Honda et al.   JOURNAL OF MEDICINAL CHEMISTRY

SCF/ -TrCP Promotes Glycogen Synthase Kinase 3-Dependent Degradation of the Nrf2 Transcription Factor in a Keap1-Independent Manner

(2011) P. Rada et al.   MOLECULAR AND CELLULAR BIOLOGY

Proteomic Analysis Shows Synthetic Oleanane Triterpenoid Binds to mTOR

(2011) Mark M. Yore et al.   PLoS One

NAD(P)H:quinone acceptor oxidoreductase 1 (NQO1), a multifunctional antioxidant enzyme and exceptionally versatile cytoprotector

(2010) Albena T. Dinkova-Kostova et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

An Exceptionally Potent Inducer of Cytoprotective Enzymes

(2010) Albena T. Dinkova-Kostova et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Keap1 perceives stress via three sensors for the endogenous signaling molecules nitric oxide, zinc, and alkenals

(2010) M. McMahon et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Loss of Nrf2 markedly exacerbates nonalcoholic steatohepatitis

(2009) Sudhir Chowdhry et al.   FREE RADICAL BIOLOGY AND MEDICINE

Activation of Nrf2-antioxidant signaling attenuates NFκB-inflammatory response and elicits apoptosis

(2008) Wenge Li et al.   BIOCHEMICAL PHARMACOLOGY

A Novel Acetylenic Tricyclic bis-(Cyano Enone) Potently Induces Phase 2 Cytoprotective Pathways and Blocks Liver Carcinogenesis Induced by Aflatoxin

(2008) K. Liby et al.   CANCER RESEARCH

Physiological Significance of Reactive Cysteine Residues of Keap1 in Determining Nrf2 Activity

(2008) T. Yamamoto et al.   MOLECULAR AND CELLULAR BIOLOGY

Coordinate regulation of enzyme markers for inflammation and for protection against oxidants and electrophiles

(2008) H. Liu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA