Direct electrophilic radiofluorination of a cyclic RGD peptide for in vivo alpha(v)beta3 integrin related tumor imaging.
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.
Ogawa
Mikako
M
Department of Biofunctional Research, National Institute for Longevity Sciences, Gengo, Morioka-cho, Obu 474-8522, Japan.
Hatano
Kentaro
K
Oishi
Shinya
S
Kawasumi
Yasuhiro
Y
Fujii
Nobutaka
N
Kawaguchi
Michiya
M
Doi
Ryuichiro
R
Imamura
Masayuki
M
Yamamoto
Mikio
M
Ajito
Keiichi
K
Mukai
Takahiro
T
Saji
Hideo
H
Ito
Kengo
K
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
D000085:Acetates; D004952:Esters; D005462:Fluorine Radioisotopes; D039302:Integrin alphaVbeta3; D019275:Radiopharmaceuticals; C040801:acetyl hypofluorite