ArticleAngewandte Chemie (International ed. in English)2019
Constrained Peptides with Fine-Tuned Flexibility Inhibit NF-Y Transcription Factor Assembly.
Article in Angewandte Chemie (International ed. in English), 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed.
- Article
- From Concepts to Inhibitors: A Blueprint for Targeting Protein-Protein Interactions.Chemical reviews · 2025Review
- Helicity-Dependent Enzymatic Peptide Cyclization.Journal of peptide science : an official publication of the European Peptide Society · 2025Article
- Flexibility-tuning of dual-display DNA-encoded chemical libraries facilitates cyclic peptide ligand discovery.Nature communications · 2025Article
- Selection of Nucleotide-Encoded Mass Libraries of Macrocyclic Peptides for Inaccessible Drug Targets.Chemical reviews · 2024Review
- Structure-Based Design and Synthesis of StapledJournal of medicinal chemistry · 2023Article
- Myo-differentiation reporter screen reveals NF-Y as an activator of PAX3-FOXO1 in rhabdomyosarcoma.Proceedings of the National Academy of Sciences of the United States of America · 2023Article
- NFYA promotes malignant behavior of triple-negative breast cancer in mice through the regulation of lipid metabolism.Communications biology · 2023Article
- Covalent Proteomimetic Inhibitor of the Bacterial FtsQB Divisome Complex.Journal of the American Chemical Society · 2022Article
- Binding of Dual-Function Hybridized MetalJACS Au · 2022Article
- Stapling of Peptides Potentiates the Antibiotic Treatment ofAntibiotics (Basel, Switzerland) · 2022Article
- Constrained peptides mimic a viral suppressor of RNA silencing.Nucleic acids research · 2021Article
- First-in-Class Cyclic Temporin L Analogue: Design, Synthesis, and Antimicrobial Assessment.Journal of medicinal chemistry · 2021Article
- NF-Y Subunits Overexpression in HNSCC.Cancers · 2021Article
- Peptide-based inhibitors of protein-protein interactions: biophysical, structural and cellular consequences of introducing a constraint.Chemical science · 2021Review
- Peptide Based Inhibitors of Protein Binding to the Mitogen-Activated Protein Kinase Docking Groove.Frontiers in molecular biosciences · 2021Article
- Article
- Stapled Peptides as HIF-1α/p300 Inhibitors: Helicity Enhancement in the Bound State Increases Inhibitory Potency.Chemistry (Weinheim an der Bergstrasse, Germany) · 2020Article
- What is the structural chemistry of the living organism at its temperature and pressure?Acta crystallographica. Section D, Structural biology · 2020Review
- Constrained Peptides with Fine-Tuned Flexibility Inhibit NF-Y Transcription Factor Assembly.Angewandte Chemie (International ed. in English) · 2019Article
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Authors and funding
10 authors.
Funding
Abstract
Protein complex formation depends on the interplay between preorganization and flexibility of the binding epitopes involved. The design of epitope mimetics typically focuses on stabilizing a particular bioactive conformation, often without considering conformational dynamics, which limits the potential of peptidomimetics against challenging targets such as transcription factors. We developed a peptide-derived inhibitor of the NF-Y transcription factor by first constraining the conformation of an epitope through hydrocarbon stapling and then fine-tuning its flexibility. In the initial set of constrained peptides, a single non-interacting α-methyl group was observed to have a detrimental effect on complex stability. Biophysical characterization revealed how this methyl group affects the conformation of the peptide in its bound state. Adaption of the methylation pattern resulted in a peptide that inhibits transcription factor assembly and subsequent recruitment to the target DNA.
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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.