Issue 16, 2012
From the journal:

Chemical Communications

A long-lived luminescent probe to sensitively detect arylamine N-acetyltransferase (NAT) activity of cells†

Takuya Terai,a   Kazuya Kikuchi,b   Yasuteru Urano,c   Hirotatsu Kojimad  and  Tetsuo Nagano*a  

* Corresponding authors

a Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan
E-mail: tlong@mol.f.u-tokyo.ac.jp
Fax: +81-3-5841-4855
Tel: +81-3-5841-4850

b Graduate School of Engineering, Osaka University, 2-1 Yamadaoka, Suita, Osaka 565-0871, Japan

c Graduate School of Medicine, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan

d Open Innovation Center for Drug Discovery, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan

Abstract

Arylamine N-acetyltransferase (NAT) is an important phase II 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 photoinduced 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.

Graphical abstract: A long-lived luminescent probe to sensitively detect arylamine N-acetyltransferase (NAT) activity of cells

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Article information

DOI
https://doi.org/10.1039/C2CC17622J
Article type
Communication
Submitted
06 Dec 2011
Accepted
05 Jan 2012
First published
17 Jan 2012

Chem. Commun., 2012,48, 2234-2236

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A long-lived luminescent probe to sensitively detect arylamine N-acetyltransferase (NAT) activity of cells

T. Terai, K. Kikuchi, Y. Urano, H. Kojima and T. Nagano, Chem. Commun., 2012, 48, 2234 DOI: 10.1039/C2CC17622J

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