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This study for the first time reports the design and application of a novel type of selective fluorescent substrate NESF for cytochrome P450 3A4 (CYP3A4) based on sulfoxidation reaction. NESF has been successfully applied for imaging endogenous CYP3A4 in living cells and for high-throughput screening of CYP3A4 inhibitors.

Graphical abstract: Discovery and evaluation of a novel selective fluorescent substrate for CYP3A4 based on sulfoxidation characteristics

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