ArticleJournal of the American Chemical Society2015
Genetically encoded fragment-based discovery of glycopeptide ligands for carbohydrate-binding proteins.
Article in Journal of the American Chemical Society, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 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
35 citing papers in PubMed, 89 citations in OpenAlex.
- Pharmacophore-driven antibody discovery on the yeast surface.bioRxiv : the preprint server for biology · 2025Article
- A Two-Step Synthesis of Covalent Genetically-Encoded Libraries of Peptide-Derived Macrocycles (cGELs) enables use of electrophiles with diverse reactivity.bioRxiv : the preprint server for biology · 2025Article
- Molecular Determinants of Affinity and Isoform Selectivity in Protein─Small Molecule Hybrid Inhibitors of Carbonic Anhydrase.Bioconjugate chemistry · 2025Article
- Late-Stage Reshaping of Phage-Displayed Libraries to Macrocyclic and Bicyclic Landscapes using a Multipurpose Linchpin.Journal of the American Chemical Society · 2025Article
- PeSTo-Carbs: Geometric Deep Learning for Prediction of Protein-Carbohydrate Binding Interfaces.Journal of chemical theory and computation · 2024Article
- Protein Engineering and High-Throughput Screening by Yeast Surface Display: Survey of Current Methods.Small science · 2023Article
- Glycomimetics for the inhibition and modulation of lectins.Chemical Society reviews · 2023Review
- Identification of specific carbonic anhydrase inhibitorsRSC medicinal chemistry · 2023Article
- Fast and Cysteine-Specific Modification of Peptides, Proteins and Bacteriophage Using Chlorooximes.Chemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
- Engineered protein-small molecule conjugates empower selective enzyme inhibition.Cell chemical biology · 2022Article
- Streamlined Iterative Assembly of Thio-Oligosaccharides by Aqueous S-Glycosylation of Diverse Deoxythio Sugars.ChemSusChem · 2022Article
- Review
- Genetically-encoded discovery of proteolytically stable bicyclic inhibitors for morphogen NODAL.Chemical science · 2021Article
- Biosynthetic Strategies for Macrocyclic Peptides.Molecules (Basel, Switzerland) · 2021Review
- Chemical Diversification of Simple Synthetic Antibodies.ACS chemical biology · 2021Article
- Identification of β-strand mediated protein-protein interaction inhibitors using ligand-directed fragment ligation.Chemical science · 2021Article
- Expanding the Chemical Diversity of Genetically Encoded Libraries.ACS combinatorial science · 2020Article
- Optimization of the Microwave Assisted Glycosylamines Synthesis Based on a Statistical Design of Experiments Approach.Molecules (Basel, Switzerland) · 2020Article
- Expanded toolbox for directing the biosynthesis of macrocyclic peptides in bacterial cells.Chemical science · 2020Article
- Mammalian lectin arrays for screening host-microbe interactions.The Journal of biological chemistry · 2020Article
Corrections and comments
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Authors and funding
17 authors at 8 institutions in 3 countries.
Funding
Abstract
We describe an approach to accelerate the search for competitive inhibitors for carbohydrate-recognition domains (CRDs). Genetically encoded fragment-based discovery (GE-FBD) uses selection of phage-displayed glycopeptides to dock a glycan fragment at the CRD and guide selection of synergistic peptide motifs adjacent to the CRD. Starting from concanavalin A (ConA), a mannose (Man)-binding protein, as a bait, we narrowed a library of 10(8) glycopeptides to 86 leads that share a consensus motif, Man-WYD. Validation of synthetic leads yielded Man-WYDLF that exhibited 40-50-fold enhancement in affinity over methyl α-d-mannopyranoside (MeMan). Lectin array suggested specificity: Man-WYD derivative bound only to 3 out of 17 proteins—ConA, LcH, and PSA—that bind to Man. An X-ray structure of ConA:Man-WYD proved that the trimannoside core and Man-WYD exhibit identical CRD docking, but their extra-CRD binding modes are significantly different. Still, they have comparable affinity and selectivity for various Man-binding proteins. The intriguing observation provides new insight into functional mimicry of carbohydrates by peptide ligands. GE-FBD may provide an alternative to rapidly search for competitive inhibitors for lectins.
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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.