ReviewMolecules (Basel, Switzerland)2018
The Keap1/Nrf2-ARE Pathway as a Pharmacological Target for Chalcones.
Review in Molecules (Basel, Switzerland), 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 60 papers.
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Who cites it
60 citing papers in PubMed, 118 citations in OpenAlex.
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- Amelioration of Fluoride Induced Toxicity by trans-Chalcone in Zebrafish Larvae and Its Gill Cell Line: An In Vivo and In Vitro Approach.Environmental toxicology · 2026Article
- Three privileged scaffolds, one pipeline: chalcones, pyrazolines and pyrazoles in drug discovery and fluorescent sensing.RSC medicinal chemistry · 2026Review
- Tanshinone IIA attenuates psoriasis via Nrf2/HO-1 activation: Mechanistic insights from preclinical models.Biochemistry and biophysics reports · 2026Article
- Design, Synthesis, and Evaluation of New Polyhydroxylated Bis-Chalcones as Potential COX-2 Selective Inhibitors.ChemMedChem · 2026Article
- The Hidden Metabolites in Glutinous Rice Huangjiu and Their Antioxidant Potential.Foods (Basel, Switzerland) · 2026Article
- Investigating the protective and therapeutic potential of new generation antioxidant combinations in the brain: an experimental aging model.Biogerontology · 2026Article
- Synthesis of (E)-3-(aryl)-1-phenylprop-2-en-1-one Chalcone Derivatives for Hyperglycemic Effect in Diabetes:Current medicinal chemistry · 2026Article
- (International journal of molecular sciences · 2025Article
- Chalcone constituents pulincisones A-F isolated from Pulicaria incisa with NQO1 inducer activity.Scientific reports · 2025Article
- Cysteine Alkylation in Enzymes and Transcription Factors: A Therapeutic Strategy for Cancer.Cancers · 2025Review
- Iturin A Potentiates Differentiation of Intestinal Epithelial Defense Cells by Modulating Keap1/Nrf2 Signaling to Mitigate Oxidative Damage Induced by Heat-Stable Enterotoxin B.Antioxidants (Basel, Switzerland) · 2025Article
- Article
- Natural products alleviate viral pneumonia by modulating inflammatory and oxidative-stress pathways.Frontiers in pharmacology · 2025Review
- Targeting Neurodegeneration: The Emerging Role of Hybrid Drugs.Current drug targets · 2025Review
- (Molecules (Basel, Switzerland) · 2024Article
- (International journal of molecular sciences · 2024Article
- Oxidative and carbonyl stress induced AMD and Codonopsis lanceolata ameliorates AMD via controlling oxidative and carbonyl stress.Scientific reports · 2024Article
- The Induction of G2/M Phase Cell Cycle Arrest and Apoptosis by the Chalcone Derivative 1C in Sensitive and Resistant Ovarian Cancer Cells Is Associated with ROS Generation.International journal of molecular sciences · 2024Article
- Michael Acceptors as Anti-Cancer Compounds: Coincidence or Causality?International journal of molecular sciences · 2024Review
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
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 the chalcones of the α,β-unsaturated carbonyl system, perceived as a potential Michael acceptor. Chalcones could activate the Kelch-like ECH-associated protein 1 (Keap1)/Nuclear factor erythroid 2-related factor 2 (Nrf2) pathway through a Michael addition reaction with the cysteines of Keap1, which acts as a redox sensor and negative regulator of Nrf2. This modification allows the dissociation of Nrf2 from the cytoplasmic complex with Keap1 and its nuclear translocation. At this level, Nrf2 binds to the antioxidant response element (ARE) and activates the expression of several detoxification, antioxidant and anti-inflammatory genes as well as genes involved in the clearance of damaged proteins. In this regard, the Keap1/Nrf2⁻ARE pathway is a new potential pharmacological target for the treatment of many chronic diseases. In this review we summarize the current progress in the study of Keap1/Nrf2⁻ARE pathway activation by natural and synthetic chalcones and their potential pharmacological applications. Among the pharmacological activities highlighted, anti-inflammatory activity was more evident than others, suggesting a multi-target Michael acceptor mechanism for the chalcones involving key regulators of the Nrf2 and nuclear factor- κB (NF-κB) pathways.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.