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

Research output: Contribution to journalArticle

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 (US)
Article numbere0130417
JournalPLoS One
Volume10
Issue number6
DOIs
StatePublished - Jun 25 2015
Externally publishedYes

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Cell-Penetrating Peptides
Furin
Proprotein Convertases
peptides
HIV-1
Human immunodeficiency virus 1
Cyclic Peptides
cells
cyclic peptides
Cell Movement
Transfection
transfection
cell movement
Peptides
drugs
Pharmaceutical Preparations
Proteins
proteins
In Vitro Techniques

ASJC Scopus subject areas

  • Agricultural and Biological Sciences(all)
  • Biochemistry, Genetics and Molecular Biology(all)
  • Medicine(all)

Cite this

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

Cationic cell-penetrating peptides are potent furin inhibitors. / Ramos-Molina, Bruno; Lick, Adam N.; Shirazi, Amir Nasrolahi; Oh, Donghoon; Tiwari, Rakesh; El-Sayed, Naglaa Salem; Parang, Keykavous; Lindberg, Iris.

In: PLoS One, Vol. 10, No. 6, e0130417, 25.06.2015.

Research output: Contribution to journalArticle

Ramos-Molina, B, Lick, AN, Shirazi, AN, Oh, D, Tiwari, R, El-Sayed, NS, Parang, K & Lindberg, I 2015, 'Cationic cell-penetrating peptides are potent furin inhibitors', PLoS One, vol. 10, no. 6, e0130417. https://doi.org/10.1371/journal.pone.0130417
Ramos-Molina B, Lick AN, Shirazi AN, Oh D, Tiwari R, El-Sayed NS et al. Cationic cell-penetrating peptides are potent furin inhibitors. PLoS One. 2015 Jun 25;10(6). e0130417. https://doi.org/10.1371/journal.pone.0130417
Ramos-Molina, Bruno ; Lick, Adam N. ; Shirazi, Amir Nasrolahi ; Oh, Donghoon ; Tiwari, Rakesh ; El-Sayed, Naglaa Salem ; Parang, Keykavous ; Lindberg, Iris. / Cationic cell-penetrating peptides are potent furin inhibitors. In: PLoS One. 2015 ; Vol. 10, No. 6.
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