title: Comparative study of the phototoxicity of long-wavelength photosensitizers targeted by the MornigaG lectin.
abstract: Morniga G is a plant lectin selective for high density of tumor-associated carbohydrate T and Tn antigens on the surface of cells. The interaction of the protein with Tn induces its cell penetration. This property was used for targeting photosensitizers (consisting of the porphyrins TrMPyP and TPPS, the Al(III)-phthalocyanin AlPcS(4), and the chlorin e6) against leukemic Jurkat T cells after covalent coupling to the protein. The control of MornigaG/photosensitizer loading allowed the comparison of the toxicity of the different photosensitizer conjugates. Conjugate including a single AlPcS(4) per protein appeared promising, since it is poorly toxic when irradiated under white light, while it shows a strong phototoxicity (LD(50) = 4 nM) when irradiated in the therapeutic window, it preferentially kills cancerous lymphocytes, and the sugar binding specificity of the lectin part of the molecule remains unaltered.
authors.affiliation: CNRS, Laboratoire de Chimie de Coordination, 205 route de Narbonne, 31077 Toulouse, France.
authors.forename: Emi
authors.initials: E
authors.lastname: Evangelio
authors.forename: Guillaume
authors.initials: G
authors.lastname: Poiroux
authors.forename: Raphaël
authors.initials: R
authors.lastname: Culerrier
authors.forename: Geneviève
authors.initials: G
authors.lastname: Pratviel
authors.forename: Els J M
authors.initials: EJ
authors.lastname: Van Damme
authors.forename: Willy J
authors.initials: WJ
authors.lastname: Peumans
authors.forename: Annick
authors.initials: A
authors.lastname: Barre
authors.forename: Pierre
authors.initials: P
authors.lastname: Rougé
authors.forename: Hervé
authors.initials: H
authors.lastname: Benoist
authors.forename: Marguerite
authors.initials: M
authors.lastname: Pitié
mesh_terms: D015295:Antigens, Tumor-Associated, Carbohydrate / Q000378:metabolism; D016923:Cell Death / Q000187:drug effects; D016503:Drug Delivery Systems; D006384:Hemagglutination / Q000187:drug effects; D006801:Humans; D019169:Jurkat Cells; D007938:Leukemia / Q000188:drug therapy*; D010778:Photochemotherapy; D017319:Photosensitizing Agents / Q000008:administration & dosage* / Q000737:chemistry* / Q000494:pharmacology; D037121:Plant Lectins / Q000737:chemistry* / Q000378:metabolism
chemical_list: D015295:Antigens, Tumor-Associated, Carbohydrate; D017319:Photosensitizing Agents; D037121:Plant Lectins; C040286:Tn antigen