Abstract

NAD(P)H: quinone oxidoreductase isozyme 1 (NQO1) is a flavoenzyme and involved in protection against oxidative stress and the regulation of metabolic functions, which is strongly implicated in neurodegenerative diseases and carcinogenic processes. Furthermore, NQO1 is also involved in the modes of action of redox-active drugs (e.g., antimalarials). Determining the activity and localization of NQO1 in living organisms is of great importance for early disease diagnosis and therapy. As a promising and convenient biosensing technique, trimethyl lock quinone-based organic molecular probes have been well established for the specific detection and imaging of NQO1 in living cells and in vivo. In this review, the recent progress of NQO1 probes based on organic small molecules is summarized from the perspectives of molecular design strategies, sensing mechanisms and bioimaging applications. We also elucidate the potential limitations and prospects of current NQO1 probes to further promote the development of versatile imaging tools for NQO1-related biomedical investigation.

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