ArticleNature communications2022
Synthesis and direct assay of large macrocycle diversities by combinatorial late-stage modification at picomole scale.
Article in Nature communications, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed.
- Beyond Simple Mimicry: Next-Generation Geometric Architectures and Future Paradigms in Small-Molecule and Macrocyclic Peptidomimetics.Angewandte Chemie (International ed. in English) · 2026Review
- High-throughput reaction screening using acoustic ejection mass spectrometry.Nature protocols · 2026Review
- Accelerate Your Science: Direct-to-Biology Strategies in Medicinal Chemistry.Journal of medicinal chemistry · 2026Review
- Synthesis of Macrocyclic Structures by Intramolecular Photoclick Reaction.Journal of the American Chemical Society · 2026Article
- Generation of membrane-permeable cyclic peptides inhibiting protein-protein interaction.Nature chemical biology · 2026Article
- Generalized Analysis of Electrophilic Small Molecules.Angewandte Chemie (International ed. in English) · 2026Article
- Massive barcode-free chemical screenings enable the discovery of bioactive macrocycles with passive membrane permeability.Nature communications · 2026Article
- Synthesis and LCMS Characterization of a 1275-Member Library of 24-Atom Triazine Macrocycles Derived from Quantitative Dimerization Occurring with >99.9% Fidelity.ACS medicinal chemistry letters · 2026Article
- Article
- Systematic Determination of the Impact of Structural Edits on Peptide Accumulation into Mycobacteria.ACS chemical biology · 2025Article
- Flexibility-tuning of dual-display DNA-encoded chemical libraries facilitates cyclic peptide ligand discovery.Nature communications · 2025Article
- Affinity selection-mass spectrometry with linearizable macrocyclic peptide libraries.Science advances · 2025Article
- Large Macrocyclic Libraries via Thioether Cyclization.Methods in molecular biology (Clifton, N.J.) · 2025Article
- Tackling Undruggable Targets with Designer Peptidomimetics and Synthetic Biologics.Chemical reviews · 2024Review
- Rapid Affinity and Microsomal Stability Ranking of Crude Mixture Libraries of Histone Deacetylase Inhibitors.ACS medicinal chemistry letters · 2024Article
- De novo development of small cyclic peptides that are orally bioavailable.Nature chemical biology · 2024Article
- Development of cyclic peptides that can be administered orally to inhibit disease targets.Nature chemical biology · 2024Article
- Are peptidomimetics the compounds of choice for developing new modulators of the JAK-STAT pathway?Frontiers in immunology · 2024Review
- MicroED as a Powerful Tool for Structure Determination of Macrocyclic Drug Compounds Directly from Their Powder Formulations.ACS chemical biology · 2023Article
- MicroED as a powerful tool for structure determination of macrocyclic drug compounds directly from their powder formulations.bioRxiv : the preprint server for biology · 2023Article
Corrections and comments
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Authors and funding
13 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Macrocycles have excellent potential as therapeutics due to their ability to bind challenging targets. However, generating macrocycles against new targets is hindered by a lack of large macrocycle libraries for high-throughput screening. To overcome this, we herein established a combinatorial approach by tethering a myriad of chemical fragments to peripheral groups of structurally diverse macrocyclic scaffolds in a combinatorial fashion, all at a picomole scale in nanoliter volumes using acoustic droplet ejection technology. In a proof-of-concept, we generate a target-tailored library of 19,968 macrocycles by conjugating 104 carboxylic-acid fragments to 192 macrocyclic scaffolds. The high reaction efficiency and small number of side products of the acylation reactions allowed direct assay without purification and thus a large throughput. In screens, we identify nanomolar inhibitors against thrombin (K
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