ArticleChembiochem : a European journal of chemical biology2017
A New Methodology for Incorporating Chiral Linkers into Stapled Peptides.
Article in Chembiochem : a European journal of chemical biology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
What it found
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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
10 citing papers in PubMed, 23 citations in OpenAlex.
- Apoptosis-inducing activity of synthetic hydrocarbon-stapled peptides in H358 cancer cells expressing KRASActa pharmaceutica Sinica. B · 2021Article
- Small and Simple, yet Sturdy: Conformationally Constrained Peptides with Remarkable Properties.International journal of molecular sciences · 2021Review
- Structural optimization of reversible dibromomaleimide peptide stapling.Peptide science (Hoboken, N.J.) · 2021Article
- Stapled Peptides-A Useful Improvement for Peptide-Based Drugs.Molecules (Basel, Switzerland) · 2019Review
- Stereoisomerism of stapled peptide inhibitors of the p53-Mdm2 interaction: an assessment of synthetic strategies and activity profiles.Chemical science · 2019Article
- The role of olefin geometry in the activity of hydrocarbon stapled peptides targeting eukaryotic translation initiation factor 4E (eIF4E).Organic & biomolecular chemistry · 2019Article
- Recognition of ASF1 by Using Hydrocarbon-Constrained Peptides.Chembiochem : a European journal of chemical biology · 2019Article
- Recent structural advances in constrained helical peptides.Medicinal research reviews · 2019Review
- Aryl transition metal chemical warheads for protein bioconjugation.Chemical science · 2018Review
- A New Methodology for Incorporating Chiral Linkers into Stapled Peptides.Chembiochem : a European journal of chemical biology · 2017Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Stapled peptides have arisen as a new class of chemical probe and potential therapeutic agents for modulating protein-protein interactions. Here, we report the first two-component i,i+7 stapling methodology that makes use of two orthogonal, on-resin stapling reactions to incorporate linkers bearing a chiral centre into a p53-derived stapled peptide. Post-stapling modifications to the chain were performed on-resin and enabled rapid access to various peptide derivatives from a single staple. The stapled peptides have increased helicity, protease stability and in vitro binding affinities to MDM2 compared to the equivalent unstapled peptide. This approach can be used to generate a library of diverse stapled peptides with different properties starting from a single stapled peptide, with scope for much greater functional diversity than that provided by existing stapling methodologies.
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What OpenQuestion holds
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.