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Updated: Mar 16, 2026

Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
Published on: September 19, 2022
Cell-Permeable Peptides Containing Cycloalanine Residues
Hao Wu1, Guillaume Mousseau2, Sonia Mediouni2
1Department of Chemistry and Cancer Biology, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL, 33458, USA.
Abstract:
We present here an efficient alternative to N-methylation for the purpose of morphing protein-binding peptides into more serum-stable and cell-permeable compounds. This involves the incorporation of a cycloalanine (CyAla) into a peptide in a way that avoids difficult coupling steps. We demonstrate the utility of this chemistry in creating a cell-permeable derivative of a high-affinity HIV Rev protein-binding peptide.
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