title: In vivo comparison of IVDU and IVFRU in HSV1-TK gene expressing tumor bearing rats.
abstract: (E)-5-(2-Iodovinyl)-2'-deoxyuridine (IVDU) and (E)-5-(2-iodovinyl)-2'-fluoro-2'-deoxyuridine (IVFRU) are potential substrates of Herpes Simplex Virus type 1 thymidine kinase (HSV-TK). In the present study, cellular uptake of radioiodinated substrates was found to be low in wild type MCA cells, but high in HSV-TK gene expressing cells. The carrier-free substrates, in particular, showed higher cellular uptake than carrier-added compounds. Biodistribution showed that the %ID/g of the MCA-TK/MCA tumor ratio of IVDU injected at 1, 4, and 24h were 1.1, 0.9 and 1.3, and those of IVFRU were 1.7, 1.7 and 1.8 respectively. Therefore, both IVDU and IVFRU could possibly be used as radiopharmaceuticals to evaluate reporter gene expression. However, IVFRU was more specific and stable than IVDU for selective non-invasive imaging of HSV-TK expression.
authors.affiliation: Laboratory of Cyclotron Application, Korea Cancer Center Hospital, and Department of Biomedical Laboratory Science, College of Health Science, Yonsei University, Seoul, South Korea.
authors.forename: Tae Hyun
authors.initials: TH
authors.lastname: Choi
authors.forename: Soon Hyuk
authors.initials: SH
authors.lastname: Ahn
authors.forename: Hee-Chung
authors.initials: HC
authors.lastname: Kwon
authors.forename: Chang Woon
authors.initials: CW
authors.lastname: Choi
authors.forename: Ok Doo
authors.initials: OD
authors.lastname: Awh
authors.forename: Sang Moo
authors.initials: SM
authors.lastname: Lim
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D016903:Drug Monitoring / Q000379:methods*; D004355:Drug Stability; D005467:Floxuridine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D015316:Genetic Therapy / Q000379:methods; D018259:Herpesvirus 1, Human / Q000201:enzymology / Q000235:genetics; D007065:Idoxuridine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D007457:Iodine Radioisotopes / Q000493:pharmacokinetics; D009369:Neoplasms / Q000628:therapy*; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D051381:Rats; D013379:Substrate Specificity; D013937:Thymidine Kinase / Q000032:analysis* / Q000235:genetics; D014018:Tissue Distribution
chemical_list: D007457:Iodine Radioisotopes; D019275:Radiopharmaceuticals; D005467:Floxuridine; C060868:5-(2-iodovinyl)-1-(2'-fluoro-2'-deoxyuridine); C030360:5-(2-iodovinyl)-2'-deoxyuridine; D013937:Thymidine Kinase; D007065:Idoxuridine