Quinone-induced activation of Keap1/Nrf2 signaling by aspirin prodrugs masquerading as nitric oxide
T Dunlap, SC Piyankarage… - Chemical research in …, 2012 - ACS Publications
The promising therapeutic potential of the NO-donating hybrid aspirin prodrugs (NO-ASA)
includes induction of chemopreventive mechanisms and has been reported in almost 100 …
includes induction of chemopreventive mechanisms and has been reported in almost 100 …
Prodrugs Bioactivated to Quinones Target NF-κB and Multiple Protein Networks: Identification of the Quinonome
EN Pierce, SC Piyankarage, T Dunlap… - Chemical research in …, 2016 - ACS Publications
Electrophilic reactive intermediates resulting from drug metabolism have been associated
with toxicity and off-target effects and in some drug discovery programs trigger NO-GO …
with toxicity and off-target effects and in some drug discovery programs trigger NO-GO …
[HTML][HTML] Small molecule deoxynyboquinone triggers alkylation and ubiquitination of Keap1 at Cys489 on Kelch domain for Nrf2 activation and inflammatory therapy
KG Linghu, T Zhang, GT Zhang, P Lv, WJ Zhang… - Journal of …, 2024 - Elsevier
Activation of nuclear factor erythroid 2-related factor 2 (Nrf2) by Kelch-like ECH-associated
protein 1 (Keap1) alkylation plays a central role in anti-inflammatory therapy. However …
protein 1 (Keap1) alkylation plays a central role in anti-inflammatory therapy. However …
Reactive sulfur species-mediated activation of the Keap1–Nrf2 pathway by 1, 2-naphthoquinone through sulfenic acids formation under oxidative stress
Y Shinkai, Y Abiko, T Ida, T Miura… - Chemical Research …, 2015 - ACS Publications
Sulfhydration by a hydrogen sulfide anion and electrophile thiolation by reactive sulfur
species (RSS) such as persulfides/polysulfides (eg, RS-SH/RS-Sn-H (R)) are unique …
species (RSS) such as persulfides/polysulfides (eg, RS-SH/RS-Sn-H (R)) are unique …
Activation of the Nrf2/ARE pathway via S-alkylation of cysteine 151 in the chemopreventive agent-sensor Keap1 protein by falcarindiol, a conjugated diacetylene …
T Ohnuma, S Nakayama, E Anan, T Nishiyama… - Toxicology and applied …, 2010 - Elsevier
Under basal conditions, the interaction of the cytosolic protein Kelch-like ECH-associated
protein 1 (Keap1) with the transcription factor nuclear factor-E2-related factor 2 (Nrf2) results …
protein 1 (Keap1) with the transcription factor nuclear factor-E2-related factor 2 (Nrf2) results …
Participation of covalent modification of Keap1 in the activation of Nrf2 by tert-butylbenzoquinone, an electrophilic metabolite of butylated hydroxyanisole
Y Abiko, T Miura, BH Phuc, Y Shinkai… - Toxicology and applied …, 2011 - Elsevier
Butylated hydroxyanisole (BHA) is an antioxidant and class-2B carcinogen. It is
biotransformed to tert-butylhydroquinone (TBHQ), which readily auto-oxidizes to the …
biotransformed to tert-butylhydroquinone (TBHQ), which readily auto-oxidizes to the …
Quinone formation as a chemoprevention strategy for hybrid drugs: balancing cytotoxicity and cytoprotection
T Dunlap, REP Chandrasena, Z Wang… - Chemical research in …, 2007 - ACS Publications
Cellular defense mechanisms that respond to damage from oxidative and electrophilic
stress, such as from quinones, represent a target for chemopreventive agents. Drugs …
stress, such as from quinones, represent a target for chemopreventive agents. Drugs …
Synthesis, evaluation, and metabolism of novel [6]-shogaol derivatives as potent Nrf2 activators
Y Zhu, P Wang, Y Zhao, C Yang, A Clark… - Free Radical Biology …, 2016 - Elsevier
Oxidative stress is a central component of many chronic diseases. The Kelch-like ECH-
associated protein 1 (Keap1)–nuclear factor erythroid 2 p45-related factor 2 (Nrf2) system is …
associated protein 1 (Keap1)–nuclear factor erythroid 2 p45-related factor 2 (Nrf2) system is …
[HTML][HTML] The Keap1/Nrf2-ARE pathway as a pharmacological target for chalcones
Chalcones have shown a broad spectrum of biological activities with clinical potential
against various diseases. The biological activities are mainly attributed to the presence in …
against various diseases. The biological activities are mainly attributed to the presence in …
[PDF][PDF] The isoquinoline PRL-295 increases the thermostability of Keap1 and disrupts its interaction with Nrf2
Transcription factor Nrf2 and its negative regulator Keap1 orchestrate a cytoprotective
response against oxidative, metabolic, and inflammatory stress. Keap1 is a drug target, with …
response against oxidative, metabolic, and inflammatory stress. Keap1 is a drug target, with …