title: Kit-like 18F-labeling of proteins: synthesis of 4-(di-tert-butyl[18F]fluorosilyl)benzenethiol (Si[18F]FA-SH) labeled rat serum albumin for blood pool imaging with PET.
abstract: Radiosyntheses of 18F-radiopharmaceuticals for positron emission tomography (PET) normally require an extraordinarily high effort of technical equipment and specially trained personnel. We recently reported a novel method for the introduction of fluorine-18 into peptides for PET-imaging based on silicon-18F-chemistry (SiFA technique). We herewith introduce the first SiFA-based Kit-like radio-fluorination of a protein (rat serum albumin,RSA) and demonstrate its usefulness for in vivo imaging with microPET in normal rats as well as in a rat heterotropic transplanted heart model. As a labeling agent, we prepared 4-(di-tert-butyl[18F]fluorosilyl)benzenethiol (Si[18F]FASH)by simple isotopic exchange in 40-60% radiochemical yield (RCY) and coupled it directly to a Sulfo-SMCC derivatized RSA in an overall RCY of 12% within 20-30 min. The technically simple labeling procedure does not require any elaborated purification procedures and is a straightforward example of a successful application of Si-18F chemistry for in vivo imaging with PET.
authors.affiliation: Department of Nuclear Medicine, Hospital of the Ludwig-Maximilians-University, Munich, Germany. bjoern.waengler@med.uni-muenchen.de
authors.forename: Björn
authors.initials: B
authors.lastname: Wängler
authors.forename: Gabriele
authors.initials: G
authors.lastname: Quandt
authors.forename: Ljuba
authors.initials: L
authors.lastname: Iovkova
authors.forename: Esther
authors.initials: E
authors.lastname: Schirrmacher
authors.forename: Carmen
authors.initials: C
authors.lastname: Wängler
authors.forename: Guido
authors.initials: G
authors.lastname: Boening
authors.forename: Marcus
authors.initials: M
authors.lastname: Hacker
authors.forename: Michael
authors.initials: M
authors.lastname: Schmoeckel
authors.forename: Klaus
authors.initials: K
authors.lastname: Jurkschat
authors.forename: Peter
authors.initials: P
authors.lastname: Bartenstein
authors.forename: Ralf
authors.initials: R
authors.lastname: Schirrmacher
mesh_terms: D000818:Animals; D005240:Feasibility Studies; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D015637:Gated Blood-Pool Imaging; D006321:Heart / Q000000981:diagnostic imaging; D017646:Organosilicon Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism*; D049268:Positron-Emission Tomography; D051381:Rats; D011933:Reagent Kits, Diagnostic; D012709:Serum Albumin / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics; D013194:Staining and Labeling / Q000379:methods*; D014018:Tissue Distribution
chemical_list: C539566:4-(di-tert-butyl(18F)fluorosilyl)benzenethiol; D005462:Fluorine Radioisotopes; D017646:Organosilicon Compounds; D011933:Reagent Kits, Diagnostic; D012709:Serum Albumin