ArticleACS combinatorial science2011
High-throughput screening of one-bead-one-compound libraries: identification of cyclic peptidyl inhibitors against calcineurin/NFAT interaction.
Article in ACS combinatorial science, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 75 citations in OpenAlex.
- Cyclic Peptides as Modulators of Protein-Protein Interactions: A Survival Guide from Discovery Platforms to AI-Driven Design.International journal of molecular sciences · 2026Review
- Article
- Tackling Undruggable Targets with Designer Peptidomimetics and Synthetic Biologics.Chemical reviews · 2024Review
- Gigavalent Display of Proteins on Monodisperse Polyacrylamide Hydrogels as a Versatile Modular Platform for Functional Assays and Protein Engineering.ACS central science · 2022Article
- Discovery of a Bicyclic Peptidyl Pan-Ras Inhibitor.Journal of medicinal chemistry · 2021Article
- Controlling Surface Wettability for Automated In Situ Array Synthesis and Direct Bioscreening.Advanced materials (Deerfield Beach, Fla.) · 2021Article
- Massively Parallel Optimization of the Linker Domain in Small Molecule Dimers Targeting a Toxic r(CUG) Repeat Expansion.ACS medicinal chemistry letters · 2021Article
- Article
- Methodologies for Backbone Macrocyclic Peptide Synthesis Compatible With Screening Technologies.Frontiers in chemistry · 2020Review
- Developments with bead-based screening for novel drug discovery.Expert opinion on drug discovery · 2019Article
- Multiplexed Competitive Screening of One-Bead-One-Component Combinatorial Libraries Using a ClonePix 2 Colony Sorter.International journal of molecular sciences · 2019Article
- Quantitative mapping of protein-peptide affinity landscapes using spectrally encoded beads.eLife · 2019Article
- Targeting the NFAT:AP-1 transcriptional complex on DNA with a small-molecule inhibitor.Proceedings of the National Academy of Sciences of the United States of America · 2019Article
- Solid-Phase Synthesis of β-Amino Ketones Via DNA-Compatible Organocatalytic Mannich Reactions.ACS combinatorial science · 2018Article
- Computational and experimental analysis of short peptide motifs for enzyme inhibition.PloS one · 2017Article
- Identification of selective covalent inhibitors of platelet activating factor acetylhydrolase 1B2 from the screening of an oxadiazolone-capped peptoid-azapeptoid hybrid library.Bioorganic & medicinal chemistry · 2016Article
- Design of a Microfluidic Chip for Magnetic-Activated Sorting of One-Bead-One-Compound Libraries.ACS combinatorial science · 2016Article
- Rapid Discovery of Functional Small Molecule Ligands against Proteomic Targets through Library-Against-Library Screening.ACS combinatorial science · 2016Article
- Machine learning assisted design of highly active peptides for drug discovery.PLoS computational biology · 2015Article
- Rapid lead discovery through iterative screening of one bead one compound libraries.ACS combinatorial science · 2015Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
One-bead-one-compound (OBOC) libraries provide a powerful tool for drug discovery as well as biomedical research. However, screening a large number of beads/compounds (>1 million) and rank ordering the initial hits (which are covalently attached to a solid support) according to their potencies still post significant technical challenges. In this work, we have integrated some of the latest technical advances from our own as well as other laboratories to develop a general methodology for rapidly screening large OBOC libraries. The methodology has been applied to synthesize and screen a cyclic peptide library that features: (1) spatially segregated beads containing cyclic peptides on the surface layer and linear encoding peptides in their interior; (2) rapid on-bead screening of the library (>1 million) by a multistage procedure (magnetic bead sorting, enzyme-linked assay, and fluorescence based screening); (3) selective release of cyclic peptides from single positive beads for solution-phase determination of their binding affinities; and (4) hit identification by partial Edman degradation/mass spectrometry (PED/MS). Screening of the library against protein phosphatase calcineurin (Cn) identified a series of cyclic peptides that bind to the substrate-docking site for nuclear factor of activated T cells (NFAT) with K(D) values of ∼1 μM. Further improvement of the affinity and specificity of these compounds may lead to a new class of immunosuppressive agents that are more selective and therefore less toxic than cyclosporine A and FK506.
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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.