ArticleChemical science2023
A cell-active cyclic peptide targeting the Nrf2/Keap1 protein-protein interaction.
Article in Chemical science, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 19 citations in OpenAlex.
- TRIM28-Derived Peptide Exerts Anti-Tumor Roles by Stabilizing Tumor Suppressive BRD7 Protein in Multiple Cancers.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- On-resin assembly of cysteine-reactive linkers for controlled site-selective antibody bioconjugation.Nature protocols · 2026Review
- Isothiocyanate-mediated cyclization of phage-displayed peptides enables discovery of macrocyclic binders.Science advances · 2026Article
- Cysteine Re-bridging Using Divinyl Pyrimidine Reagents for the Generation of Antibody-Drug Conjugates.Methods in molecular biology (Clifton, N.J.) · 2026Article
- Fragment-Based Drug Discovery of Novel High-affinity, Selective, and Anti-inflammatory Inhibitors of the Keap1-Nrf2 Protein-Protein Interaction.Angewandte Chemie (International ed. in English) · 2025Article
- Bioinformatics-Assisted Discovery of Antioxidant Cyclic Peptides from Corn Gluten Meal.Foods (Basel, Switzerland) · 2025Article
- Proteostasis Decline and Redox Imbalance in Age-Related Diseases: The Therapeutic Potential of NRF2.Biomolecules · 2025Review
- RoseTTAFold diffusion-guided short peptide design: a case study of binders against Keap1/Nrf2.Computational and structural biotechnology journal · 2025Article
- Tackling Undruggable Targets with Designer Peptidomimetics and Synthetic Biologics.Chemical reviews · 2024Review
- A facile strategy for the construction of a phage display cyclic peptide library for the selection of functional macrocycles.Chemical science · 2024Article
- De novo antioxidant peptide design via machine learning and DFT studies.Scientific reports · 2024Article
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 2 countries.
Funding
Abstract
The disruption of the protein-protein interaction (PPI) between Nrf2 and Keap1 is an attractive strategy to counteract the oxidative stress that characterises a variety of severe diseases. Peptides represent a complementary approach to small molecules for the inhibition of this therapeutically important PPI. However, due to their polar nature and the negative net charge required for binding to Keap1, the peptides reported to date exhibit either mid-micromolar activity or are inactive in cells. Herein, we present a two-component peptide stapling strategy to rapidly access a variety of constrained and functionalised peptides that target the Nrf2/Keap1 PPI. The most promising peptide, P8-H containing a fatty acid tag, binds to Keap1 with nanomolar affinity and is effective at inducing transcription of ARE genes in a human lung epithelial cell line at sub-micromolar concentration. Furthermore, crystallography of the peptide in complex with Keap1 yielded a high resolution X-ray structure, adding to the toolbox of structures available to develop cell-permeable peptidomimetic inhibitors.
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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.