ArticleChemistryOpen2017
De Novo Modular Development of a Foldameric Protein-Protein Interaction Inhibitor for Separate Hot Spots: A Dynamic Covalent Assembly Approach.
Article in ChemistryOpen, 2017. 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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11 citing papers in PubMed, 30 citations in OpenAlex.
- De Novo Design of Multivalent α/β-Peptides Mimicking Transcription Factors Targeting the CBP KIX Domain.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
- Light-Driven Competitive Selection in a Protein-Catalyzed Dissipative Peptide Replication.Angewandte Chemie (International ed. in English) · 2026Article
- Betaine-Conjugated ß-Peptide Foldamers: Influence of Quaternary Charge on Self-Organization and MorphologyFormation.ChemistryOpen · 2025Article
- Chirality Effects in Peptide-Based Dynamic Combinatorial Chemistry.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- Harnessing Aromatic-Histidine Interactions through Synergistic Backbone Extension and Side Chain Modification.Angewandte Chemie (International ed. in English) · 2023Article
- Light-Fueled Primitive Replication and Selection in Biomimetic Chemical Systems.Journal of the American Chemical Society · 2023Article
- Promiscuity mapping of the S100 protein family using a high-throughput holdup assay.Scientific reports · 2022Article
- Proteomimetic surface fragments distinguish targets by function.Chemical science · 2020Article
- NMR Spectroscopy of supramolecular chemistry on protein surfaces.Beilstein journal of organic chemistry · 2020Review
- Dynamic Covalent Chemistry of Aldehyde Enamines: BiChemistry (Weinheim an der Bergstrasse, Germany) · 2017Article
- De Novo Modular Development of a Foldameric Protein-Protein Interaction Inhibitor for Separate Hot Spots: A Dynamic Covalent Assembly Approach.ChemistryOpen · 2017Article
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Protein-protein interactions stabilized by multiple separate hot spots are highly challenging targets for synthetic scaffolds. Surface-mimetic foldamers bearing multiple recognition segments are promising candidate inhibitors. In this work, a modular bottom-up approach is implemented by identifying short foldameric recognition segments that interact with the independent hot spots, and connecting them through dynamic covalent library (DCL) optimization. The independent hot spots of a model target (calmodulin) are mapped with hexameric β-peptide helices using a pull-down assay. Recognition segment hits are subjected to a target-templated DCL ligation through thiol-disulfide exchange. The most potent derivative displays low nanomolar affinity towards calmodulin and effectively inhibits the calmodulin-TRPV1 interaction. The DCL assembly of the folded segments offers an efficient approach towards the de novo development of a high-affinity inhibitor of protein-protein interactions.
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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.