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Structure-guided design enables development of a hyperpolarized molecular probe for detection of aminopeptidase N activity in vivo
https://repo.qst.go.jp/records/85020
https://repo.qst.go.jp/records/85020fe97d66a-0104-433b-9826-cb8c3d613257
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2021-04-19 | |||||
| タイトル | ||||||
| タイトル | Structure-guided design enables development of a hyperpolarized molecular probe for detection of aminopeptidase N activity in vivo | |||||
| 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 |
Saito, Yutaro
× Saito, Yutaro× Yatabe, Hiroyuki× Tamura, Iori× Kondo, Yohei× Ishida, Ryo× Seki, Tomohiro× Hiraga, Keita× Eguchi, Akihiro× Takakusagi, Yoichi× Saito, Keisuke× Oshima, Nobu× Ishikita, Hiroshi× Yamamoto, Kazutoshi× C. Krishna, Murali× Sando, Shinsuke× Yoichi, Takakusagi |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Dynamic nuclear polarization (DNP) is a cutting-edge technique that dramatically enhances the detection sensitivity of molecules using nuclear magnetic resonance imaging (NMR/MRI). This methodology enables real-time imaging of dynamic metabolic status in vivo using MRI. To expand the targetable metabolic reactions, there is a demand for developing exogenous, i.e., artificially designed, DNP-NMR molecular probes; however, complying with the requirements of practical DNP-NMR molecular probes is challenging due to the lack of established design guidelines. Herein, we report Ala-[1-13C]Gly-d2-NMe2 as a DNP-NMR molecular probe for in vivo detection of aminopeptidase N (APN) activity. We developed this probe rationally through precise structural investigation, calculation, biochemical assessment, and advanced molecular design to achieve rapid and detectable responses to enzyme activity in vivo. With the fabricated probe, we successfully detected enzymatic activity in vivo. This report presents a comprehensive approach for the development of artificially derived, practical DNP-NMR molecular probes through structure-guided molecular design. | |||||
| 書誌情報 |
Sci Adv 巻 8, 号 13, 発行日 2022-03 |
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| 出版者 | ||||||
| 出版者 | AAAS | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 2375-2548 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1126/sciadv.abj2667 | |||||
| 関連サイト | ||||||
| 識別子タイプ | URI | |||||
| 関連識別子 | https://www.science.org/doi/10.1126/sciadv.abj2667 | |||||
