ChemMedChem
ChemMedChem
5 years ago

(R-X-R)4-motif peptides containing conformationally constrained cyclohexane-derived spacers: Effect on cellular uptake

Govind S Bhosle, Moneesha Fernandes
Arginine-rich peptides having the (R-X-R)n- motif are among the most effective cell-penetrating peptides. Here, we report several fold increase in the efficacy of such CPPs when the linear flexible spacer (-X-) in the (R-X-R) motif is replaced by constrained cyclic 1,4-cyclohexane-derived spacers. Internalization of these oligomers in mammalian cell lines was found to be an energy-dependent process. Incorporation of these constrained, non-proteinogenic amino acid spacers in the CPPs is shown to enhance their proteolytic stability.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1002/cmdc.201700498

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