TY - JOUR
T1 - Cationic cell-penetrating peptides are potent furin inhibitors
AU - Ramos-Molina, Bruno
AU - Lick, Adam N.
AU - Shirazi, Amir Nasrolahi
AU - Oh, Donghoon
AU - Tiwari, Rakesh
AU - El-Sayed, Naglaa Salem
AU - Parang, Keykavous
AU - Lindberg, Iris
PY - 2015/6/25
Y1 - 2015/6/25
N2 - 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.
AB - 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.
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U2 - 10.1371/journal.pone.0130417
DO - 10.1371/journal.pone.0130417
M3 - Article
C2 - 26110264
AN - SCOPUS:84938283574
SN - 1932-6203
VL - 10
JO - PLoS One
JF - PLoS One
IS - 6
M1 - e0130417
ER -