ArticleJournal of medicinal chemistry2025
Backbone Alterations in Cyclic Peptides Influence Both Membrane Permeability and Biological Activity.
Article in Journal of medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
3 citing papers in PubMed.
- Dynamics of (Hetero)aryl Motifs: An Integrative Approach To Study the Conformational Landscape in Macrocycles.Journal of the American Chemical Society · 2026Article
- Scaling SMILES-based chemical language models for therapeutic peptide engineering.bioRxiv : the preprint server for biology · 2026Article
- Recent Advances in Cyclic Peptide-Based Therapeutic Strategies for Renal Cell Carcinoma: A Focused Review.Drug design, development and therapy · 2026Review
Corrections and comments
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Authors and funding
7 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Cyclic peptides hold significant potential as disruptors of challenging targets such as protein-protein interactions, but their poor passive membrane permeability limits their use. In this study, we used a combination of cell-permeability assays and a target-agnostic cell-painting assay to observe how minimal structural changes affect membrane permeability and the biological activity of Sanguinamide A analogues. Significant differences in permeability were observed among the analogues, and for those that were permeable, NMR spectroscopy revealed conformational changes in response to environmental polarity. In the cell-painting assay, we observed that even though permeability generally correlated with overall morphological changes, distinct differences in specific activities were observed depending on the nature of the backbone modification. These findings highlight the importance of selecting the correct backbone modification when trying to balance both membrane permeability and biological activity, offering valuable insights for the development of cyclic peptides as therapeutic agents.
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Registered trials
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