In vivo targeting of hydrogen peroxide by activatable cell-penetrating peptides

Roy Weinstain, Elamprakash N. Savariar, Csilla N. Felsen, Roger Y. Tsien*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

218 Scopus citations

Abstract

A hydrogen peroxide (H2O2)-activated cell-penetrating peptide was developed through incorporation of a boronic acid-containing cleavable linker between polycationic cell-penetrating peptide and polyanionic fragments. Fluorescence labeling of the two ends of the molecule enabled monitoring its reaction with H2O2 through release of the highly adhesive cell-penetrating peptide and disruption of fluorescence resonance energy transfer. The H2O2 sensor selectively reacts with endogenous H2O2 in cell culture to monitor the oxidative burst of promyelocytes and in vivo to image lung inflammation. Targeting H2O2 has potential applications in imaging and therapy of diseases related to oxidative stress.

Original languageEnglish
Pages (from-to)874-877
Number of pages4
JournalJournal of the American Chemical Society
Volume136
Issue number3
DOIs
StatePublished - 22 Jan 2014
Externally publishedYes

Funding

FundersFunder number
Howard Hughes Medical Institute
National Institutes of Health5R01CA158448-02, 5R25CA153915-03
U.S. Department of DefenseW81XWH-09-1-0699
National Cancer InstituteR01CA158448

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