title: Porphyrin-bile acid conjugates: from saccharide recognition in the solution to the selective cancer cell fluorescence detection.
abstract: This paper describes the preparation and use of conjugates of porphyrins and bile acids as ligands to bind to tumor expressed saccharides. Bile acid-porphyrin conjugates were tested for recognition of saccharides that are typically present on malignant tumor cells. Fluorescence microscopy, in vitro PDT cell killing, and PDT of subcutaneous 4T1 mouse tumors is reported. High selectivity for saccharide cancer markers and cancer cells was observed. This in vivo and in vitro study demonstrated high potential use for these compounds in targeted photodynamic therapy.
authors.affiliation: Institute of Molecular Genetics, Academy of Sciences of the Czech Republic, Videnska 1083, 14220 Prague 4, Czech Republic. kralova@img.cas.cz
authors.forename: Jarmila
authors.initials: J
authors.lastname: Králová
authors.forename: Juha
authors.initials: J
authors.lastname: Koivukorpi
authors.forename: Zdenek
authors.initials: Z
authors.lastname: Kejík
authors.forename: Pavla
authors.initials: P
authors.lastname: Poucková
authors.forename: Elina
authors.initials: E
authors.lastname: Sievänen
authors.forename: Erkki
authors.initials: E
authors.lastname: Kolehmainen
authors.forename: Vladimír
authors.initials: V
authors.lastname: Král
mesh_terms: D016475:3T3 Cells; D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D001647:Bile Acids and Salts / Q000737:chemistry* / Q000494:pharmacology; D001665:Binding Sites; D014408:Biomarkers, Tumor / Q000032:analysis*; D002241:Carbohydrates / Q000737:chemistry*; D002460:Cell Line; D002461:Cell Line, Transformed; D049109:Cell Proliferation / Q000187:drug effects; D053938:DNA Fragmentation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006031:Glycosylation; D006367:HeLa Cells; D006801:Humans; D008024:Ligands; D051379:Mice; D008807:Mice, Inbred BALB C; D008856:Microscopy, Fluorescence / Q000379:methods; D015394:Molecular Structure; D009369:Neoplasms / Q000175:diagnosis* / Q000188:drug therapy; D010778:Photochemotherapy / Q000379:methods; D011166:Porphyrins / Q000737:chemistry* / Q000494:pharmacology; D012680:Sensitivity and Specificity; D012996:Solutions / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D001647:Bile Acids and Salts; D014408:Biomarkers, Tumor; D002241:Carbohydrates; D008024:Ligands; D011166:Porphyrins; D012996:Solutions