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Design, Synthesis, and Biological Evaluation of Novel Fluorescent Probes Targeting the 18 kDa Translocator Protein
https://repo.qst.go.jp/records/82774
https://repo.qst.go.jp/records/827749fc20abb-2c84-4016-9480-2dca16b14b06
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2021-03-03 | |||||
| タイトル | ||||||
| タイトル | Design, Synthesis, and Biological Evaluation of Novel Fluorescent Probes Targeting the 18 kDa Translocator 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 |
Wongso, Hendris
× Wongso, Hendris× Tomoteru, Yamasaki× Katsushi, Kumata× Maiko, Ono× Makoto, Higuchi× Zhang, Ming-Rong× Fulham, Michael× Katsifis, Andrew× Anthony Keller, Paul× Tomoteru, Yamasaki× Katsushi, Kumata× Maiko, Ono× Makoto, Higuchi× Zhang, Ming-Rong |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | A series of fluorescent probes from the 6-chloro-2-phenylimidazo[1,2- a ]pyridine-3-yl acetamides ligands featuring the 7-nitro-2-oxa-1,3-diazol-4-yl (NBD) moiety were synthesized and biologically evaluated for their fluorescence properties and for their binding affinity to the 18 kDa translocator protein (TSPO). Spectroscopic studies including UV-Vis absorption and fluorescence measurements showed that the synthesized fluorescent probes exhibit favorable spectroscopic properties, especially in non-polar environments . In vitro fluorescence staining in the brain sections from lipopolysaccharide (LPS)-injected mice revealed partial colocalization of probes with the TSPO. The TSPO binding affinity of probes was measured on crude mitochondrial fractions separated from rat brain homogenates using [ 11 C]PK11195 radioligand binding assay. All the new fluorescent probes demonstrated moderate to high binding affinity to the TSPO, with affinity ( K i ) values ranging from 0.58 nM to 3.28 µM. Taking these data together, we propose that the new fluorescent probes could be used to visualize the TSPO. Keywords: TSPO; fluorescent probes; imaging; neurodegenerative diseases. |
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| 書誌情報 |
ChemMedChem 巻 16, 号 12, p. 1902-1916, 発行日 2021-02 |
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| 出版者 | ||||||
| 出版者 | WILEY | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 1860-7187 | |||||
| PubMed番号 | ||||||
| 識別子タイプ | PMID | |||||
| 関連識別子 | 33631047 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1002/cmdc.202000984 | |||||
| 関連サイト | ||||||
| 識別子タイプ | URI | |||||
| 関連識別子 | https://chemistry-europe.onlinelibrary.wiley.com/doi/abs/10.1002/cmdc.202000984 | |||||
