期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 59, 期 35, 页码 15147-15151出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202004094
关键词
diagnostics; melanoma; selenium probes; seminaphthorhodafluor; thioredoxin reductase
资金
- National Institutes of Health [R15EB016870]
- NIH [P41-GM103311]
We report the first diselenide-based probe for the selective detection of thioredoxin reductase (TrxR), an enzyme commonly overexpressed in melanomas. The probe design involves conjugation of a seminaphthorhodafluor dye with a diselenide moiety. TrxR reduces the diselenide bond, triggering a fluorescence turn-on response of the probe. Kinetic studies reveal favorable binding of the probe with TrxR with a Michaelis-Menten constant (K-m) of 15.89 mu m. Computational docking simulations predict a greater binding affinity to the TrxR active site in comparison to its disulfide analogue. In vitro imaging studies further confirmed the diselenide probe exhibited improved signaling of TrxR activity compared to the disulfide analogue.
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