title: Internalization of Near-Infrared Fluorescently Labeled Activatable Cell-Penetrating Peptide and of Proteins into Human Fibrosarcoma Cell Line HT-1080.
abstract: The internalization of near-infrared fluorescently labeled cargos into living cells and tissues allows a highly sensitive detection without interference from skin, porphins or other fluorescent cell and tissue compounds. In this study, the uptake of labeled bovine serum albumin and an antibody, into fibrosarcoma (HT-1080) cells was triggered by the formation of non-covalent complexes with different cell-penetrating peptides; uptake efficiency and intracellular localization were determined. To improve selectivity of internalization into tumor cells, a fluorescent activatable cell-penetrating peptide (ACPP) was synthesized and functionally characterized. This 25-mer peptide was designed to be activatable by Matrix-Metallo-Proteases (MMPs). Its uptake selectivity was estimated using cells with different MMP activities.
authors.affiliation: Institute of Diagnostic and Interventional Radiology, Department of Experimental Radiology, Jena University Hospital, Friedrich-Schiller University, Erlanger Allee 101, Jena, 07747, Germany.
authors.forename: Felista
authors.initials: F
authors.lastname: Tansi
authors.affiliation: Institute of Diagnostic and Interventional Radiology, Department of Experimental Radiology, Jena University Hospital, Friedrich-Schiller University, Erlanger Allee 101, Jena, 07747, Germany.|Ernst-Abbe-University of Applied Sciences, Carl-Zeiss-Promenade 2, Jena, 07745, Germany.
authors.forename: Eric
authors.initials: E
authors.lastname: Kallweit
authors.affiliation: Leibniz Institute for Age Research, Fritz-Lipmann-Institute, Beutenbergstr. 11, Jena, 07745, Germany.
authors.forename: Christoph
authors.initials: C
authors.lastname: Kaether
authors.affiliation: Jena Bioscience GmbH, Loebstedter Str. 80, Jena, 07749, Germany.
authors.forename: Katarina
authors.initials: K
authors.lastname: Kappe
authors.affiliation: Ernst-Abbe-University of Applied Sciences, Carl-Zeiss-Promenade 2, Jena, 07745, Germany.
authors.forename: Christina
authors.initials: C
authors.lastname: Schumann
authors.affiliation: Institute of Diagnostic and Interventional Radiology, Department of Experimental Radiology, Jena University Hospital, Friedrich-Schiller University, Erlanger Allee 101, Jena, 07747, Germany.
authors.forename: Ingrid
authors.initials: I
authors.lastname: Hilger
authors.affiliation: Jena Bioscience GmbH, Loebstedter Str. 80, Jena, 07749, Germany.|Centrum of Molecular Biomedicine, Institute of Biochemistry and Biophysics, Friedrich- Schiller-University, Dornburger Str. 25, Jena, 07743, Germany.
authors.forename: Siegmund
authors.initials: S
authors.lastname: Reissmann
mesh_terms: D002232:Carbocyanines / Q000737:chemistry*; D045744:Cell Line, Tumor; D057846:Cell-Penetrating Peptides / Q000138:chemical synthesis / Q000494:pharmacology*; D016503:Drug Delivery Systems / Q000379:methods; D005456:Fluorescent Dyes / Q000737:chemistry; D006801:Humans; D007211:Indoles / Q000737:chemistry*; D020782:Matrix Metalloproteinases / Q000378:metabolism; D012710:Serum Albumin, Bovine / Q000737:chemistry*; D000068878:Trastuzumab / Q000737:chemistry* / Q000378:metabolism
chemical_list: D002232:Carbocyanines; D057846:Cell-Penetrating Peptides; C573549:DY-676; D005456:Fluorescent Dyes; D007211:Indoles; D012710:Serum Albumin, Bovine; D020782:Matrix Metalloproteinases; D000068878:Trastuzumab
keywords: ACTIVATION BY MATRIX-METALLO-PROTEASES; BOVINE SERUM ALBUMIN; CAD-2; CELL-PENETRATING PEPTIDES; CPP-DEPENDENT UPTAKE EFFICIENCY; FORMATION OF NON-COVALENT COMPLEXES BETWEEN CARGO AND CPP; HISTONES; HIV-TAT (47-57); HUMAN FIBROSARCOMA HT-1080 CELLS; INTRACELLULAR TRAFFICKING; MPGalpha; MPGbeta; NEAR INFRARED FLUORESCENT LABELED CARGOS; PROTEODUCIN; SELECTIVITY OF INTERNALIZATION