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PET study on mice bearing human colon adenocarcinoma cells using [11C]GF120918, a dual radioligand for P-glycoprotein and breast cancer resistance protein
https://repo.qst.go.jp/records/45951
https://repo.qst.go.jp/records/45951b426cc24-a6da-4f3b-89cf-6f0bf08878f0
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2010-12-03 | |||||
| タイトル | ||||||
| タイトル | PET study on mice bearing human colon adenocarcinoma cells using [11C]GF120918, a dual radioligand for P-glycoprotein and breast cancer resistance protein | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
| 資源タイプ | journal article | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Yamasaki, Tomoteru
× Yamasaki, Tomoteru× Kawamura, Kazunori× Hatori, Akiko× Yui, Joji× Yanamoto, Kazuhiko× Yoshida, Yuichiro× Ogawa, Masanao× Nengaki, Nobuki× Wakizaka, Hidekatsu× Fukumura, Toshimitsu× Zhang, Ming-Rong× 山崎 友照× 河村 和紀× 羽鳥 晶子× 由井 譲二× 柳本 和彦× 吉田 勇一郎× 小川 政直× 念垣 信樹× 脇坂 秀克× 福村 利光× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Objective: To evaluate the functions of P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) in human colon adenocarcinoma (Caco-2), we carried out an in-vitro study and a small animal positron emission tomography (PET) study using [11C]GF120918 (elacridar). \nMethods: [11C]GF120918 was synthesized by reacting the desmethyl precursor with [11C]CH3I. An in-vitro study using [11C]GF120918 was carried out in Caco-2 and Madin–Darby canine kidney cells in the presence or absence of a transporter inhibitor (cyclosporine A and unlabeled GF120918). The biodistribution of radioactivity after the injection of [11C]GF120918 was determined in Caco-2-bearing mice using a small animal PET scanner. \nResults: In Caco-2 cells expressing Pgp and BCRP, coincubation with unlabeled GF120918 caused an approximately two-fold increase in [11C]GF120918 uptake compared with that of the control ([11C]GF120918 only). In Caco-2-bearing mice, PET results indicated that [11C]GF120918 uptake in the tumor was low, but was significantly increased by treatment with unlabeled GF120918. In metabolite analysis, the radioactive component in the tumor almost corresponded to intact [11C]GF120918. \nConclusion: A PET study combining the administration of [11C]GF120918 with unlabeled GF120918 may be a useful tool for evaluating the functions of Pgp and BCRP in tumors. |
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| 書誌情報 |
Nuclear Medicine Communications 巻 31, 号 11, p. 985-993, 発行日 2010-11 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0143-3636 | |||||
