ArticleACS chemical biology2021
Parallel Screening Using the Chloroalkane Penetration Assay Reveals Structure-Penetration Relationships.
Article in ACS chemical biology, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
- Click-based determination of accumulation of molecules in Escherichia coli.Nature communications · 2026Article
- Recent advances in methods for quantifying the cell penetration of macromolecules.Current opinion in chemical biology · 2024Review
- Comparing Cell Penetration of Biotherapeutics across Human Cell Lines.ACS chemical biology · 2024Article
- Investigating the Cytosolic Delivery of Proteins by Lipid Nanoparticles Using the Chloroalkane Penetration Assay.Biochemistry · 2024Article
- Cell-permeable chameleonic peptides: Exploiting conformational dynamics in de novo cyclic peptide design.Current opinion in structural biology · 2023Review
- Liposomal Permeation Assay for Droplet-Scale Pharmacokinetic Screening.Journal of medicinal chemistry · 2023Article
- Quantitative Analysis and Optimization of Site-Specific Protein Bioconjugation in Mammalian Cells.Bioconjugate chemistry · 2022Article
- Investigation of Carboxylic Acid Isosteres and Prodrugs for Inhibition of the Human SIRT5 Lysine Deacylase Enzyme.Angewandte Chemie (International ed. in English) · 2022Article
Corrections and comments
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Authors and funding
3 authors.
Funding
Abstract
The efficiency with which polycationic peptides penetrate the cytosol depends on the number and overall patterning of arginine residues. While general trends and unusually penetrant patterns of arginine residues have been discovered, prior work has not effectively leveraged high-throughput screens to measure cytosolic penetration rather than total cell uptake. In this work, we adapted the chloroalkane penetration assay, which exclusively measures cytosolic penetration, to screen peptide libraries in a high-throughput, quantitative, and automation-ready manner. We demonstrate the usefulness of the screening platform by efficiently exploring how the number, patterning, and stereochemistry of arginine residues affect the cytosolic penetration of a model 10-residue peptide.
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Registered trials
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