Related Experiment Video
Updated: Apr 17, 2026
Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
Published on: September 19, 2022
Enhanced serum proteolysis resistance of cell-penetrating peptides
Jesús Fominaya1, Jerónimo Bravo, Didier Decaudin
1CIMI-Paris, UPMC UMRS CR7-Inserm U1135-CNRS ERL 8255, Faculte de Medicine Pierre et Marie Curie, CHU Pitié Salpêtrière, 91, Bd de 1-Hôpital, 75013 Paris, France.
Aim:
Before starting preclinical studies, we have analyzed the integrity in serum of DPT-C9h, a promising therapeutic peptide, and performed modifications in order to improve its stability.
Materials & Methods:
Mutant peptides exchanging arginine 8 for either lysine, asparagine or alanine were synthesized and compared with the parental peptide.
Results:
All mutants clearly improved peptide stability while keeping their functional activity. PK studies showed an enhanced stability, being Mut3DPT-C9h the most promising candidate. Biodistribution studies demonstrate that the modified peptide is able to reach the targeted tumor and accumulate there at higher concentration than the parental peptide.
Discussion:
Small modifications in the peptide sequence result in improvements allowing the selection of better candidates for preclinical studies.
