Cationic cell-penetrating peptides are potent furin inhibitors

Bruno Ramos-Molina, Adam N. Lick, Amir Nasrolahi Shirazi, Donghoon Oh, Rakesh Tiwari, Naglaa Salem El-Sayed, Keykavous Parang, Iris Lindberg

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14 Scopus citations

Abstract

Cationic cell-penetrating peptides have been widely used to enhance the intracellular delivery of various types of cargoes, such as drugs and proteins. These reagents are chemically similar to the multi-basic peptides that are known to be potent proprotein convertase inhibitors. Here, we report that both HIV-1 TAT47-57 peptide and the Chariot reagent are micromolar inhibitors of furin activity in vitro. In agreement, HIV-1 TAT47-57 reduced HT1080 cell migration, thought to be mediated by proprotein convertases, by 25%. In addition, cyclic polyarginine peptides containing hydrophobic moieties which have been previously used as transfection reagents also exhibited potent furin inhibition in vitro and also inhibited intracellular convertases. Our finding that cationic cell-penetrating peptides exert potent effects on cellular convertase activity should be taken into account when biological effects are assessed.

Original languageEnglish
Article numbere0130417
JournalPloS one
Volume10
Issue number6
DOIs
StatePublished - Jun 25 2015
Externally publishedYes

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    Ramos-Molina, B., Lick, A. N., Shirazi, A. N., Oh, D., Tiwari, R., El-Sayed, N. S., Parang, K., & Lindberg, I. (2015). Cationic cell-penetrating peptides are potent furin inhibitors. PloS one, 10(6), [e0130417]. https://doi.org/10.1371/journal.pone.0130417