期刊
CHEMICAL COMMUNICATIONS
卷 48, 期 16, 页码 2234-2236出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c2cc17622j
关键词
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资金
- Ministry of Education, Culture, Sports, Science and Technology of Japan [22000006, 23651231]
- New Energy and Industrial Technology Development Organization (NEDO) of Japan
- Cosmetology Research Foundation
- Mochida Memorial Foundation for Medical and Pharmaceutical Research, Japan
- Grants-in-Aid for Scientific Research [22000006, 23651231] Funding Source: KAKEN
Arylamine N-acetyltransferase (NAT) is an important phase 11 metabolizing enzyme that influences drug efficacy and adverse effects. Here, we report a long-lived luminescent lanthanide complex as a probe for NAT, employing an intraligand photo-induced electron transfer strategy. The probe shows approximately 100-fold increase of luminescence upon N-acetylation catalyzed by NAT, with relatively high specificity for NAT2 over NAT1. It is the first NAT probe that is suitable for sensitive, homogeneous, and rapid detection of NAT activity of recombinant enzyme or cell lysate, and is expected to be useful for drug discovery and clinical diagnosis.
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