title: Direct electrophilic radiofluorination of a cyclic RGD peptide for in vivo alpha(v)beta3 integrin related tumor imaging.
abstract: The association of the alpha(v)beta(3) integrin with tumor metastasis and tumor related angiogenesis has been suggested. Therefore, by imaging the alpha(v)beta(3) receptor with PET, information concerning the tumor status could be obtained. Cyclic peptides including the RGD sequence, were radiolabeled by direct electrophilic fluorination with [(18)F]AcOF. In tumor-bearing mice, the labeled peptides accumulated at the tumor with a high tumor to blood ratio. These findings suggest that an assessment of tumor characteristics may be obtained by using these (18)F-labeled peptides.
authors.affiliation: Department of Biofunctional Research, National Institute for Longevity Sciences, Gengo, Morioka-cho, Obu 474-8522, Japan.
authors.forename: Mikako
authors.initials: M
authors.lastname: Ogawa
authors.forename: Kentaro
authors.initials: K
authors.lastname: Hatano
authors.forename: Shinya
authors.initials: S
authors.lastname: Oishi
authors.forename: Yasuhiro
authors.initials: Y
authors.lastname: Kawasumi
authors.forename: Nobutaka
authors.initials: N
authors.lastname: Fujii
authors.forename: Michiya
authors.initials: M
authors.lastname: Kawaguchi
authors.forename: Ryuichiro
authors.initials: R
authors.lastname: Doi
authors.forename: Masayuki
authors.initials: M
authors.lastname: Imamura
authors.forename: Mikio
authors.initials: M
authors.lastname: Yamamoto
authors.forename: Keiichi
authors.initials: K
authors.lastname: Ajito
authors.forename: Takahiro
authors.initials: T
authors.lastname: Mukai
authors.forename: Hideo
authors.initials: H
authors.lastname: Saji
authors.forename: Kengo
authors.initials: K
authors.lastname: Ito
mesh_terms: D000085:Acetates / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics; D000230:Adenocarcinoma / Q000000981:diagnostic imaging* / Q000378:metabolism*; D000818:Animals; D001415:Back / Q000000981:diagnostic imaging; D003110:Colonic Neoplasms / Q000000981:diagnostic imaging / Q000378:metabolism; D004952:Esters / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics; D005462:Fluorine Radioisotopes / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D006801:Humans; D007275:Injections, Intravenous; D039302:Integrin alphaVbeta3 / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D007553:Isotope Labeling / Q000379:methods; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D009368:Neoplasm Transplantation; D009928:Organ Specificity; D010084:Oxidation-Reduction; D019275:Radiopharmaceuticals / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics; D012680:Sensitivity and Specificity; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed / Q000379:methods
chemical_list: D000085:Acetates; D004952:Esters; D005462:Fluorine Radioisotopes; D039302:Integrin alphaVbeta3; D019275:Radiopharmaceuticals; C040801:acetyl hypofluorite