Table of Contents
Int. J. Mol. Sci., Volume 21, Issue 20 (October-2 2020) – 377 articles
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Cover Story (view full-size image) New hybrid γ/γ-peptides, consisting of a cyclobutane-containing amino acid joined in alternation to [...] Read more. New hybrid γ/γ-peptides, consisting of a cyclobutane-containing amino acid joined in alternation to a cis- or trans-γ-amino-L-proline decorated with guanidinium groups, have been synthesized and evaluated both as cell-penetrating peptides and as selective drug delivery vectors on Leishmania. While they lacked cytotoxicity on the tumoral human cell line HeLa, the tetradecamers were active on the protozoan parasite Leishmania with significant intracellular accumulation. Their conjugates with doxorubicin (Dox) improved the leishmanicidal effect of the free drug. Through molecular dynamics, the Dox moiety becomes wrapped by the peptide chain to be secluded from the aqueous environment, while the solubility of this payload increases by the exposed guanidinium groups at the periphery of the conjugate. View this paper