title: Biodistribution, Stability, and Blood Distribution of the Cell Penetrating Peptide Maurocalcine in Mice.
abstract: Maurocalcine (MCa) is the first natural cell penetrating peptide to be discovered in animal venom. In addition to the fact that it represents a potent vector for the cell penetration of structurally diverse therapeutic compounds, MCa also displays several distinguishing features that make it a potential peptide of choice for clinical and biotechnological applications. The aim of the present study was to gain new information about the properties of MCa in vivo in order to delineate the future potential applications of this vector. For this purpose, two analogues of this peptide with (Tyr-MCa) and without (Lin-Tyr-MCa) disulfide bridges were synthesized, radiolabeled with (125)I, and their in vitro stabilities were first evaluated in mouse blood. The results indicated that (125)I-Tyr-MCa was stable in vitro and that the disulfide bridges conferred a competitive advantage for the stability of peptide. Following in vivo injection in mice, (125)I-Tyr-MCa targeted peripheral organs with interesting quantitative differences and the main route of peptide elimination was renal.
authors.affiliation: Grenoble Alpes University, 38041 Saint-Martin-d'Hères, France. pascale.perret@ujf-grenoble.fr.|Radiopharmaceutiques Biocliniques, INSERM, UMR S1039, 38700 La Tronche, France. pascale.perret@ujf-grenoble.fr.
authors.forename: Pascale
authors.initials: P
authors.lastname: Perret
authors.affiliation: Grenoble Alpes University, 38041 Saint-Martin-d'Hères, France. mitra.ahmadi@ujf-grenoble.fr.|Radiopharmaceutiques Biocliniques, INSERM, UMR S1039, 38700 La Tronche, France. mitra.ahmadi@ujf-grenoble.fr.
authors.forename: Mitra
authors.initials: M
authors.lastname: Ahmadi
authors.affiliation: Grenoble Alpes University, 38041 Saint-Martin-d'Hères, France. laurent.riou@ujf-grenoble.fr.|Radiopharmaceutiques Biocliniques, INSERM, UMR S1039, 38700 La Tronche, France. laurent.riou@ujf-grenoble.fr.
authors.forename: Laurent
authors.initials: L
authors.lastname: Riou
authors.affiliation: Grenoble Alpes University, 38041 Saint-Martin-d'Hères, France. sandrine.bacot@ujf-grenoble.fr.|Radiopharmaceutiques Biocliniques, INSERM, UMR S1039, 38700 La Tronche, France. sandrine.bacot@ujf-grenoble.fr.
authors.forename: Sandrine
authors.initials: S
authors.lastname: Bacot
authors.affiliation: Smartox Biotechnologies, Bâtiment Nanobio, 570 rue de la Chimie, 38400 Saint Martin d'Hères, France. julien.pecher@gmail.com.
authors.forename: Julien
authors.initials: J
authors.lastname: Pecher
authors.affiliation: Grenoble Alpes University, 38041 Saint-Martin-d'Hères, France. cathy.poillot@gmail.com.|Science and Therapeutics, LabEx Ion Channels, Grenoble Institute of Neuroscience, INSERM, U836, 38700 La Tronche, France. cathy.poillot@gmail.com.
authors.forename: Cathy
authors.initials: C
authors.lastname: Poillot
authors.affiliation: Grenoble Alpes University, 38041 Saint-Martin-d'Hères, France. alexis.broisat@inserm.fr.|Radiopharmaceutiques Biocliniques, INSERM, UMR S1039, 38700 La Tronche, France. alexis.broisat@inserm.fr.
authors.forename: Alexis
authors.initials: A
authors.lastname: Broisat
authors.affiliation: Grenoble Alpes University, 38041 Saint-Martin-d'Hères, France. catherine.ghezzi@ujf-grenoble.fr.|Radiopharmaceutiques Biocliniques, INSERM, UMR S1039, 38700 La Tronche, France. catherine.ghezzi@ujf-grenoble.fr.
authors.forename: Catherine
authors.initials: C
authors.lastname: Ghezzi
authors.affiliation: Grenoble Alpes University, 38041 Saint-Martin-d'Hères, France. dewaardm@ujf-grenoble.fr.|Smartox Biotechnologies, Bâtiment Nanobio, 570 rue de la Chimie, 38400 Saint Martin d'Hères, France. dewaardm@ujf-grenoble.fr.|Science and Therapeutics, LabEx Ion Channels, Grenoble Institute of Neuroscience, INSERM, U836, 38700 La Tronche, France. dewaardm@ujf-grenoble.fr.
authors.forename: Michel
authors.initials: M
authors.lastname: De Waard
mesh_terms: D000818:Animals; D057846:Cell-Penetrating Peptides / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D004355:Drug Stability; D007553:Isotope Labeling; D051379:Mice; D049268:Positron-Emission Tomography; D012604:Scorpion Venoms / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D014018:Tissue Distribution; D055114:X-Ray Microtomography
chemical_list: D057846:Cell-Penetrating Peptides; D012604:Scorpion Venoms; C406406:maurocalcine
keywords: blood stability; cell-penetrating peptide; drug delivery; in vivo biodistribution; maurocalcine