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Can I read Development of a Cyclic, Cell Penetrating Peptide Compatible with In Vitro Selection Strategies on EtoBox?
Development of a Cyclic, Cell Penetrating Peptide Compatible with In Vitro Selection Strategies by Nicolas A. Abrigo; Kara K. Dods; Chelsea A. Makovsky; Sandeep Lohan; Koushambi Mitra; Kaylee M. Newcomb; Anthony Le; Matthew C. T. Hartman is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Development of a Cyclic, Cell Penetrating Peptide Compatible with In Vitro Selection Strategies about?
A key limitation for the development of peptides as therapeutics is their lack of cell permeability. Recent work has shown that short, arginine-rich macrocyclic peptides containing hydrophobic amino acids are able to penetrate cells and reach the cytosol. Here, we have developed a new strategy for developing cyclic cell penetrating peptides (CPPs) that shifts some of the hydrophobic character to the peptide cyclization linker, allowing us to do a linker screen to find cyclic CPPs with improved cellular uptake. We demonstrate that both hydrophobicity and position of the alkylation points on the linker affect uptake of macrocyclic cell penetrating peptides (CPPs). Our best peptide, 4i, is on par with or better than prototypical CPPs Arg 9 (R9) and CPP12 under assays measuring total cellular uptake and cytosolic delivery. 4i was also able to carry a peptide previously discovered from an in vitro selection, 8.6, and a cytotoxic peptide into the cytosol. A bicyclic variant of 4i showed even better cytosolic entry than 4i, highlighting the plasticity of this class of peptides toward modifications. Since our CPPs are cyclized via their side chains (as opposed to head-to-tail cyclization),
Who reads Development of a Cyclic, Cell Penetrating Peptide Compatible with In Vitro Selection Strategies?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Nicolas A. Abrigo; Kara K. Dods; Chelsea A. Makovsky; Sandeep Lohan; Koushambi Mitra; Kaylee M. Newcomb; Anthony Le; Matthew C. T. Hartman
- Publisher
- American Chemical Society (ACS)
- Published
- 2023
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)