ArticleFrontiers in pharmacology2015
Optimization of the cyclotide framework to improve cell penetration properties.
Article in Frontiers in pharmacology, 2015. 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, 44 citations in OpenAlex.
- Computational screening of AI-derived cyclotides as putative VEGFR2 binders for wound-site angiogenesis.Scientific reports · 2026Article
- Small and Versatile Cyclotides as Anti-infective Agents.ACS infectious diseases · 2025Review
- Kalata B1 Enhances Temozolomide Toxicity to Glioblastoma Cells.Biomedicines · 2024Article
- On chip microfluidic separation of cyclotides.Turkish journal of chemistry · 2023Article
- Comparison of a Short Linear Antimicrobial Peptide with Its Disulfide-Cyclized and Cyclotide-Grafted Variants against Clinically Relevant Pathogens.Microorganisms · 2021Article
- Harnessing cyclotides to design and develop novel peptide GPCR ligands.RSC chemical biology · 2020Review
- Discovery and mechanistic studies of cytotoxic cyclotides from the medicinal herbThe Journal of biological chemistry · 2020Article
- Cellular Uptake and Cytosolic Delivery of a Cyclic Cystine Knot Scaffold.ACS chemical biology · 2020Article
- Emerging Methods and Design Principles for Cell-Penetrant Peptides.Angewandte Chemie (International ed. in English) · 2018Review
- Designing macrocyclic disulfide-rich peptides for biotechnological applications.Nature chemical biology · 2018Article
- Chemical Synthesis and Functional Analysis of VarvA Cyclotide.Molecules (Basel, Switzerland) · 2018Article
- β-Ginkgotides: Hyperdisulfide-constrained peptides from Ginkgo biloba.Scientific reports · 2017Article
- A current perspective on applications of macrocyclic-peptide-based high-affinity ligands.Biopolymers · 2016Review
- Design of substrate-based BCR-ABL kinase inhibitors using the cyclotide scaffold.Scientific reports · 2015Article
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
Cell penetrating peptides have been regarded as promising vectors to deliver hydrophilic molecules inside cells. Although they are great tools for research and have high potential as drug delivery systems, their application as drugs is impaired by their low stability in serum. Cyclotides, cyclic disulfide-rich peptides from plants, are ultra-stable molecules that have inspired applications in drug design as they can be used as scaffolds to stabilize linear bioactive sequences. Recently, they have also been shown to possess cell-penetrating properties. The combination of their remarkable stability and cell-penetrating properties opens new avenues for the application of peptides to bind to and inhibit intracellular proteins. Nevertheless, for a broader application of these molecules as vectors is of utmost importance to improve their cellular internalization efficiency. In this study we successfully modified MCoTI-II, one of the most widely studied cyclotide scaffolds in drug design, and improved its internalization properties. The internalization of the newly designed MCoTI-II is as efficient as the gold standard cell-penetrating peptide (CPP) TAT and maintains all the required features as a template to graft desired bioactivities.
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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.