title: Novel chemoselective (18)F-radiolabeling of thiol-containing biomolecules under mild aqueous conditions.
abstract: We report a novel prosthetic group based on a heterocyclic methylsulfone derivative for the rapid, stable, and chemoselective (18)F-labeling of thiol-containing (bio)molecules under mild aqueous reaction conditions. Compared to established maleimide approaches, the new methodology displays some clear advantages for imaging probe development.
authors.affiliation: Center for Radiopharmaceutical Sciences ETH-PSI-USZ, Institute of Pharmaceutical Sciences ETH, Vladimir-Prelog Weg 4, CH-8093 Zurich, Switzerland. t.mindt@gmx.ch.
authors.forename: Aristeidis
authors.initials: A
authors.lastname: Chiotellis
authors.forename: Filippo
authors.initials: F
authors.lastname: Sladojevich
authors.forename: Linjing
authors.initials: L
authors.lastname: Mu
authors.forename: Adrienne
authors.initials: A
authors.lastname: Müller Herde
authors.forename: Ibai E
authors.initials: IE
authors.lastname: Valverde
authors.forename: Vladimir
authors.initials: V
authors.lastname: Tolmachev
authors.forename: Roger
authors.initials: R
authors.lastname: Schibli
authors.forename: Simon M
authors.initials: SM
authors.lastname: Ametamey
authors.forename: Thomas L
authors.initials: TL
authors.lastname: Mindt
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D005462:Fluorine Radioisotopes / Q000737:chemistry; D006801:Humans; D007553:Isotope Labeling; D008301:Maleimides / Q000737:chemistry; D051379:Mice; D008819:Mice, Nude; D009369:Neoplasms / Q000175:diagnosis / Q000000981:diagnostic imaging; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D013438:Sulfhydryl Compounds / Q000737:chemistry*; D014018:Tissue Distribution; D014183:Transplantation, Heterologous; D014867:Water / Q000737:chemistry*
chemical_list: D005462:Fluorine Radioisotopes; D008301:Maleimides; D019275:Radiopharmaceuticals; D013438:Sulfhydryl Compounds; D014867:Water; C043592:maleimide