title: In vivo targeting of hydrogen peroxide by activatable cell-penetrating peptides.
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.
authors.affiliation: Department of Pharmacology, ‡Department of Chemistry and Biochemistry, and §Howard Hughes Medical Institute, University of California San Diego , La Jolla, California 92093, United States.
authors.forename: Roy
authors.initials: R
authors.lastname: Weinstain
authors.forename: Elamprakash N
authors.initials: EN
authors.lastname: Savariar
authors.forename: Csilla N
authors.initials: CN
authors.lastname: Felsen
authors.forename: Roger Y
authors.initials: RY
authors.lastname: Tsien
mesh_terms: D015374:Biosensing Techniques / Q000379:methods*; D001897:Boronic Acids / Q000737:chemistry / Q000378:metabolism; D002470:Cell Survival; D057846:Cell-Penetrating Peptides / Q000378:metabolism*; D018922:HL-60 Cells; D006801:Humans; D006861:Hydrogen Peroxide / Q000378:metabolism*; D057054:Molecular Imaging
chemical_list: D001897:Boronic Acids; D057846:Cell-Penetrating Peptides; D006861:Hydrogen Peroxide