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Design strategy for serine hydroxymethyltransferase probes based on retro-aldol-type reaction
https://repo.qst.go.jp/records/75744
https://repo.qst.go.jp/records/75744260bc632-257b-4307-8f0a-3e8613f0fbac
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2019-04-26 | |||||
| タイトル | ||||||
| タイトル | Design strategy for serine hydroxymethyltransferase probes based on retro-aldol-type reaction | |||||
| 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 |
Nonaka, Hiroshi
× Nonaka, Hiroshi× Nakanishi, Yuki× Kuno, Satoshi× Ota, Tomoki× Mochidome, Kentaro× Saito, Yutaro× Sugihara, Fuminori× Takakusagi, Yoichi× Aoki, Ichio× Nagatoishi, Satoru× Tsumoto, Kouhei× Sando, Shinsuke× Takakusagi, Yoichi× Aoki, Ichio |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Serine hydroxymethyltransferase (SHMT) is an enzyme that catalyzes the reaction that converts serine to glycine. It plays an important role in one-carbon metabolism. Recently, SHMT has been shown to be associated with various diseases. Therefore, SHMT has attracted attention as a biomarker and drug target. However, the development of molecular probes responsive to SHMT has not yet been realized. This is because SHMT catalyzes an essential yet simple reaction; thus, the substrates that can be accepted into the active site of SHMT are limited. Here, we focus on the SHMT-catalyzed retro-aldol reaction rather than the canonical serine–glycine conversion and succeed in developing fluorescent and 19F NMR molecular probes. Taking advantage of the facile and direct detection of SHMT, the devel- oped fluorescent probe is used in the high-throughput screening for human SHMT inhibitors, and two hit compounds are obtained. | |||||
| 書誌情報 |
Nature Communications 巻 10, 号 1, p. 876, 発行日 2019-02 |
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| 出版者 | ||||||
| 出版者 | Nature.com | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 2041-1723 | |||||
| PubMed番号 | ||||||
| 識別子タイプ | PMID | |||||
| 関連識別子 | 30787298 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1038/s41467-019-08833-7 | |||||
| 関連サイト | ||||||
| 識別子タイプ | URI | |||||
| 関連識別子 | https://www.nature.com/articles/s41467-019-08833-7 | |||||
