title: Efficient cellular delivery of β-galactosidase mediated by NrTPs, a new family of cell-penetrating peptides.
abstract: Nucleolar targeting peptides (NrTPs), a recently developed family of cell-penetrating peptides, have been shown to be very efficient in entering cells and accumulating in their nucleoli. In this work, we have used conjugates of NrTP6 (YKQSHKKGGKKGSG) covalently linked to β-galactosidase in order to demonstrate the capacity of NrTP for intracellular delivery of large molecules. NrTP6/β-galactosidase conjugates, prepared by maleimide-based chemistry, were stable and enzymatically active on the standard 4-methylumbelliferyl β-d-galactopyranoside substrate. Their translocation into HeLa cells, monitored by β-galactosidase activity as a readout of the uptake, showed efficient cellular entry and thus demonstrated the potential of NrTPs for intracellular delivery of large-size cargos with preservation of biological activity.
authors.affiliation: Instituto de Medicina Molecular, Faculdade de Medicina da Universidade de Lisboa, Lisbon, Portugal.
authors.forename: Margarida
authors.initials: M
authors.lastname: Rodrigues
authors.forename: Beatriz G
authors.initials: BG
authors.lastname: de la Torre
authors.forename: Gandhi
authors.initials: G
authors.lastname: Rádis-Baptista
authors.forename: Nuno C
authors.initials: NC
authors.lastname: Santos
authors.forename: David
authors.initials: D
authors.lastname: Andreu
mesh_terms: D000595:Amino Acid Sequence; D057846:Cell-Penetrating Peptides / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D006367:HeLa Cells; D006801:Humans; D008958:Models, Molecular; D008969:Molecular Sequence Data; D015394:Molecular Structure; D021381:Protein Transport / Q000502:physiology; D001616:beta-Galactosidase / Q000737:chemistry* / Q000378:metabolism
chemical_list: D057846:Cell-Penetrating Peptides; D001616:beta-Galactosidase