Cationic Cell-Penetrating Peptides Are Potent Furin Inhibitors

Authors

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

Document Type

Article

Publication Date

6-25-2015

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.

Comments

This article was originally published in PLoS ONE, volume 10, issue 6, in 2015. DOI: 10.1371/journal.pone.0130417

Recommended Citation

Ramos-Molina B, Lick AN, Nasrolahi Shirazi A, Oh D, Tiwari R, El-Sayed NS, et al. (2015) Cationic Cell-Penetrating Peptides Are Potent Furin Inhibitors. PLoS ONE 10(6): e0130417. doi:10.1371/ journal.pone.0130417

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The authors

Creative Commons License

This work is licensed under a Creative Commons Attribution 4.0 License.