ArticleChembiochem : a European journal of chemical biology2015
Rapid parallel synthesis of bioactive folded cyclotides by using a tea-bag approach.
Article in Chembiochem : a European journal of chemical biology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 26 citations in OpenAlex.
- Tackling Undruggable Targets with Designer Peptidomimetics and Synthetic Biologics.Chemical reviews · 2024Review
- Resistance is futile: targeting multidrug-resistant bacteria withRSC chemical biology · 2023Review
- Lipidation of a bioactive cyclotide-based CXCR4 antagonist greatly improves its pharmacokinetic profile in vivo.Journal of controlled release : official journal of the Controlled Release Society · 2023Article
- Insights into the synthesis strategies of plant-derived cyclotides.Amino acids · 2023Review
- Using the Cyclotide Scaffold for Targeting Biomolecular Interactions in Drug Development.Molecules (Basel, Switzerland) · 2022Review
- Engineered Cyclotides with Potent Broad in Vitro and in Vivo Antimicrobial Activity.Chemistry (Weinheim an der Bergstrasse, Germany) · 2021Article
- The Potential of the Cyclotide Scaffold for Drug Development.Biomedicines · 2019Review
- Using backbone-cyclized Cys-rich polypeptides as molecular scaffolds to target protein-protein interactions.The Biochemical journal · 2019Review
- Cyclotides, a versatile ultrastable micro-protein scaffold for biotechnological applications.Bioorganic & medicinal chemistry letters · 2017Review
- In vivo Evaluation of an Engineered Cyclotide as Specific CXCR4 Imaging Reagent.Chemistry (Weinheim an der Bergstrasse, Germany) · 2017Article
- Cyclotides: Overview and Biotechnological Applications.Chembiochem : a European journal of chemical biology · 2017Review
- Full Sequence Amino Acid Scanning of θ-Defensin RTD-1 Yields a Potent Anthrax Lethal Factor Protease Inhibitor.Journal of medicinal chemistry · 2017Article
- Chemical and biological production of cyclotides.Advances in botanical researchArticle
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
We report here the first rapid parallel production of bioactive folded cyclotides by using Fmoc-based solid-phase peptide synthesis in combination with a "tea-bag" approach. Using this approach, we efficiently synthesized 15 analogues of the CXCR4 antagonist cyclotide MCo-CVX-5c. Cyclotides were synthesized in a single-pot, cyclization/folding reaction in the presence of reduced glutathione. Natively folded cyclotides were quickly purified from the cyclization/folding crude mixture by activated thiol Sepharose-based chromatography. The different folded cyclotide analogues were then tested for their ability to inhibit the CXCR4 receptor in a cell-based assay. The results indicated that this approach can be used for the efficient chemical synthesis of libraries of cyclotides with improved biological properties that can be easily interfaced with solution or cell-based assays for rapid screening.
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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.