ArticleNature chemical biology2009
Phage-encoded combinatorial chemical libraries based on bicyclic peptides.
Article in Nature chemical biology, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 296 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
296 citing papers in PubMed, 726 citations in OpenAlex.
- De Novo Discovery of Nonstandard Thioisoindole-Bridged Bicyclic Peptides Targeting Traf2- and NCK-Interacting Kinase.Angewandte Chemie (International ed. in English) · 2026Article
- Anticancer Peptides: Design Principles, Translational Bottlenecks, and Emerging Opportunities.Molecules (Basel, Switzerland) · 2026Review
- Bacterial Display of Genetically Encoded Macrocyclic Peptide Libraries Using Cysteine-Reactive Unnatural Amino Acids.ACS chemical biology · 2026Article
- Sortase-mediated generation of various macrocyclic peptide scaffolds from low-reactivity electrophilic substrates.Chemical science · 2026Article
- Genetically Encoded Lysine-Selective Photocyclization Enables Phage Display Selection of Cyclic Peptide Binders.Angewandte Chemie (International ed. in English) · 2026Article
- Organometallic Chemistry Approach to Peptide Tricycles.Bioconjugate chemistry · 2026Article
- Advances in Cyclic Peptides Targeting G Protein-Coupled Receptors.Chembiochem : a European journal of chemical biology · 2026Review
- Phage Display as a Promising Platform for Peptide Drug Discovery.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Discovery of Noninhibitory Macrocyclic Ligands for Protein Tyrosine Phosphatase 1B Using a Function-Based, Iterative Screening Strategy.Journal of the American Chemical Society · 2026Article
- Tetrazine-Enabled Peptide Macrocyclization and Bioorthogonal Cell Penetration Profiling.JACS Au · 2026Article
- Genetically Encoding Propiolamide Warhead for the Construction of Phage Displayed Cyclic Peptide Library.Chembiochem : a European journal of chemical biology · 2026Article
- Peptides as programmable molecular scaffolds: from chemical synthesis and engineering to translational medicine.RSC chemical biology · 2026Review
- Article
- A plasmid toolbox for the easy autodisplay of recombinant proteins and its optimization.Communications biology · 2026Article
- Triple threat bismuth peptide imaging in cells.Chemical science · 2026Article
- Massive barcode-free chemical screenings enable the discovery of bioactive macrocycles with passive membrane permeability.Nature communications · 2026Article
- Linker Engineering in Stapled Peptides for Enhanced Membrane Permeability: Screening and Optimization Strategies.International journal of molecular sciences · 2026Review
- Discovering Serum Stable Protein-Protein Interaction Inhibitors with N‑Terminus-Capped Bicyclic Phage Libraries.JACS Au · 2026Article
- Unlocking the potential of EphA2 with precision-guided cancer therapy: bicycle drug conjugates.Journal of translational medicine · 2026Review
- Bismuth Bicycles.Journal of peptide science : an official publication of the European Peptide Society · 2026Review
236 more citing papers are in PubMed but not listed here.
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
Here we describe a phage strategy for the selection of ligands based on bicyclic or linear peptides attached covalently to an organic core. We designed peptide repertoires with three reactive cysteine residues, each spaced apart by several random amino acid residues, and we fused the repertoires to the phage gene-3-protein. Conjugation with tris-(bromomethyl)benzene via the reactive cysteines generated repertoires of peptide conjugates with two peptide loops anchored to a mesitylene core. Iterative affinity selections yielded several enzyme inhibitors; after further mutagenesis and selection, we were able to chemically synthesize a lead inhibitor (PK15; Ki =1.5 nM) specific to human plasma kallikrein that efficiently interrupted the intrinsic coagulation pathway in human plasma tested ex vivo. This approach offers a powerful means of generating and selecting bicyclic macrocycles (or if cleaved, linear derivatives thereof) as ligands poised at the interface of small-molecule drugs and biologics.
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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.