ArticleScience advances2019
Thiol-to-amine cyclization reaction enables screening of large libraries of macrocyclic compounds and the generation of sub-kilodalton ligands.
Article in Science advances, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed.
- Accelerate Your Science: Direct-to-Biology Strategies in Medicinal Chemistry.Journal of medicinal chemistry · 2026Review
- Article
- Tackling Undruggable Targets with Designer Peptidomimetics and Synthetic Biologics.Chemical reviews · 2024Review
- A facile strategy for the construction of a phage display cyclic peptide library for the selection of functional macrocycles.Chemical science · 2024Article
- De novo development of small cyclic peptides that are orally bioavailable.Nature chemical biology · 2024Article
- Article
- Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows.bioRxiv : the preprint server for biology · 2023Article
- High-Throughput Platform for Novel Reaction Discovery.Chemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
- Synthesis and direct assay of large macrocycle diversities by combinatorial late-stage modification at picomole scale.Nature communications · 2022Article
- Macrocyclization strategies for cyclic peptides and peptidomimetics.RSC medicinal chemistry · 2021Review
- A Eu(III)-based Metal Organic Framework: Selective Sensing of Picric Acid and Nursing Application Values On the Cerebral Edema Induced by Cerebral Hemorrhage Via Reducing the Coagulation Factor II Activity.Journal of fluorescence · 2021Article
- Strategies to expand peptide functionality through hybridisation with a small molecule component.RSC chemical biology · 2021Review
- Shedding Light on the Molecular Recognition of Sub-Kilodalton Macrocyclic Peptides on Thrombin by Supervised Molecular Dynamics.Frontiers in molecular biosciences · 2021Article
- Macrocycle synthesis strategy based on step-wise "adding and reacting" three components enables screening of large combinatorial libraries.Chemical science · 2020Article
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Authors and funding
15 authors.
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Abstract
Macrocyclic compounds are an attractive modality for drug development, but the limited availability of large, structurally diverse macrocyclic libraries hampers the discovery of leads. Here, we describe the discovery of efficient macrocyclization reactions based on thiol-to-amine ligations using bis-electrophiles, their application to synthesize and screen large libraries of macrocyclic compounds, and the identification of potent small macrocyclic ligands. The thiol-to-amine cyclization reactions showed unexpectedly high yields for a wide substrate range, which obviated product purification and enabled the generation and screening of an 8988 macrocycle library with a comparatively small effort. X-ray structure analysis of an identified thrombin inhibitor (
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