ArticleAngewandte Chemie (International ed. in English)2022
Biocompatible and Selective Generation of Bicyclic Peptides.
Article in Angewandte Chemie (International ed. in English), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
What it found
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The trial behind it
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Who cites it
14 citing papers in PubMed, 36 citations in OpenAlex.
- Macrocyclization of native peptides through (thio)urea crosslinking of two amines.Nature communications · 2026Article
- Folded-state compatibility and unfolded-state constraint govern staple-based stabilization: guidelines from a coiled-coil model.RSC chemical biology · 2026Article
- Overcoming Methicillin-ResistantResearch (Washington, D.C.) · 2026Article
- Differential Self-Assembly Behaviors and Proteolytic Stability of Bicyclic Peptides Compared to Monocyclic Peptides.Chemistry, an Asian journal · 2026Article
- Bismuth-Selenopeptides Combine Potent Bioactivity with Exceptional Kinetic Inertness.Angewandte Chemie (International ed. in English) · 2025Article
- Discovery of Pyrazole-3-Carboxylic Acid Derivatives as Dengue Virus Protease Inhibitors with Antiviral Activity.ACS medicinal chemistry letters · 2025Article
- Advances in Peptidomimetics for Next-Generation Therapeutics: Strategies, Modifications, and Applications.Chemical reviews · 2025Review
- Metallo-azapeptides: Controlled Metal Chelation to Peptide Backbone Nitrogen.Journal of the American Chemical Society · 2025Article
- Nitrile-aminothiol bioorthogonal near-infrared fluorogenic probes for ultrasensitive in vivo imaging.Nature communications · 2025Article
- Recent Advances in Metal-Free Peptide Stapling Strategies.Chem & bio engineering · 2024Review
- Biocompatible strategies for peptide macrocyclisation.Chemical science · 2024Review
- Development and Challenges of Cyclic Peptides for Immunomodulation.Current protein & peptide science · 2024Review
- Biocompatible and Selective Generation of Bicyclic Peptides.Angewandte Chemie (International ed. in English) · 2022Article
- Site-selective generation of lanthanoid binding sites on proteins using 4-fluoro-2,6-dicyanopyridine.Magnetic resonance (Gottingen, Germany) · 2022Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Bicyclic peptides possess superior properties for drug discovery; however, their chemical synthesis is not straightforward and often neither biocompatible nor fully orthogonal to all canonical amino acids. The selective reaction between 1,2-aminothiols and 2,6-dicyanopyridine allows direct access to complex bicyclic peptides in high yield. The process can be fully automated using standard solid-phase peptide synthesis. Bicyclization occurs in water at physiological pH within minutes and without the need for a catalyst. The use of various linkers allows tailored bicyclic peptides with qualities such as plasma stability, conformational preorganization, and high target affinity. We demonstrate this for a bicyclic inhibitor of the Zika virus protease NS2B-NS3 as well as for bicyclic versions of the α-helical antimicrobial peptide aurein 1.2.
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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.