ArticleProtein science : a publication of the Protein Society2013
Development of a steady-state FRET-based assay to identify inhibitors of the Keap1-Nrf2 protein-protein interaction.
Article in Protein science : a publication of the Protein Society, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 32 citations in OpenAlex.
- Function-based OBOC screening for the direct discovery of potent protein-protein interaction inhibitors.RSC chemical biology · 2026Article
- Peptides as programmable molecular scaffolds: from chemical synthesis and engineering to translational medicine.RSC chemical biology · 2026Review
- Biophysical and Biochemical Assays for Screening Small Molecule Inhibitors Targeting Toxin-Ribosome Interactions.Toxins · 2026Review
- A novel mRNA decay inhibitor abolishes pathophysiological cellular transition.Cell death discovery · 2022Article
- Development of a Homogeneous Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) Assay for the Inhibition of Keap1-Nrf2 Protein-Protein Interaction.SLAS discovery : advancing life sciences R & D · 2021Article
- Beyond repression of Nrf2: An update on Keap1.Free radical biology & medicine · 2020Review
- Development of an enzyme-linked immunosorbent assay for Keap1-Nrf2 interaction inhibitors identification.Redox biology · 2020Article
- Nrf2 activation through the inhibition of Keap1-Nrf2 protein-protein interaction.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2020Article
- Emerging Screening Approaches in the Development of Nrf2-Keap1 Protein-Protein Interaction Inhibitors.International journal of molecular sciences · 2019Review
- Exploring new strategies for grafting binding peptides onto protein loops using a consensus-designed tetratricopeptide repeat scaffold.Protein science : a publication of the Protein Society · 2019Article
- Astroglia as a cellular target for neuroprotection and treatment of neuro-psychiatric disorders.Glia · 2017Review
- Structural Basis of the Inhibition of STAT1 Activity by Sendai Virus C Protein.Journal of virology · 2015Article
- Nrf2--a therapeutic target for the treatment of neurodegenerative diseases.Free radical biology & medicine · 2015Review
- Non-electrophilic modulators of the canonical Keap1/Nrf2 pathway.Bioorganic & medicinal chemistry letters · 2015Review
- Monitoring Keap1-Nrf2 interactions in single live cells.Biotechnology advances · 2014Review
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
One of the strategies proposed for the chemoprevention of degenerative diseases and cancer involves upregulation of antioxidant and free radical detoxification gene products by increasing the intracellular concentration of the transcription factor nuclear factor erythroid 2-related factor 2 (Nrf2). This can be achieved by disrupting the interaction between Nrf2 and Kelch-like ECH associated protein 1 (Keap1), a substrate adaptor protein for a Cul3-dependent E3 ubiquitin ligase complex. Here, we describe the development of a high-throughput fluorescence (or Förster) resonance energy transfer assay for the identification of inhibitors of the Keap1-Nrf2 protein-protein interaction (PPI). The basis of this assay is the binding of a YFP-conjugated Keap1 Kelch binding domain to a CFP-conjugated Nrf2-derived 16-mer peptide containing a highly conserved "ETGE" motif. The competition aspect of the assay was validated using unlabeled Nrf2-derived 7-mer and 16-mer peptides and has potential as a screening tool for small molecule inhibitors of the PPI. We discuss the development of this assay in the context of other methods used to evaluate this PPI.
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Registered trials
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.