WEKO3
アイテム
Synthesis and evaluation of 11C-labeled coumarin analog as an imaging probe for detecting monocarboxylate transporters expression
https://repo.qst.go.jp/records/48405
https://repo.qst.go.jp/records/484057c31932d-fecb-4d40-89dc-4f7793f1ce8a
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2017-12-06 | |||||
| タイトル | ||||||
| タイトル | Synthesis and evaluation of 11C-labeled coumarin analog as an imaging probe for detecting monocarboxylate transporters expression | |||||
| 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 |
Tateishi, Hiroyuki
× Tateishi, Hiroyuki× Tsuji, Atsushi× Kato, Koichi× Sudo, Hitomi× Sugyo, Aya× Hanakawa, Takashi× Zhang, Ming-Rong× Saga, Tsuneo× Yasushi, Arano× Higashi, Tatsuya× 立石 裕行× 辻 厚至× 加藤 孝一× 須藤 仁美× 須尭 綾× 張 明栄× 佐賀 恒夫× 東 達也 |
|||||
| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Upregulated monocarboxylate transporters (MCTs) in tumors are considered diagnostic imaging targets. Herein, we synthesized the positron emission tomography probe candidates coumarin analogs 2 and 3, and showed 55 times higher affinity of 2 for MCTs than a representative MCT inhibitor. Whereas [11C] 2 showed low tumor accumulation, probably due to adduct formation with plasma proteins, [11C]2 showed high initial brain uptake, suggesting that the scaffold of 2 has properties that are preferable in imaging probes for the astrocyte–neuron lactate shuttle. Although further optimization of 2 is required, our findings can be used to inform the development of MCT-targeted imaging agents. 2017 The Author(s). Published by Elsevier Ltd. This is an open access article under the CC BY license |
|||||
| 書誌情報 |
Bioorganic & Medicinal Chemistry Letters 巻 27, 号 21, p. 4893-4897, 発行日 2017-09 |
|||||
| 出版者 | ||||||
| 出版者 | Elsevier | |||||
| PubMed番号 | ||||||
| 識別子タイプ | PMID | |||||
| 関連識別子 | 28951078 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1016/j.bmcl.2017.09.033 | |||||
