二硒醚
硫氧还蛋白还原酶
化学
荧光
转身(生物化学)
硫氧还蛋白
酶
生物化学
硒
光学
有机化学
物理
作者
Tendai J. Mafireyi,Madeleine Laws,John W. Bassett,Pamela B. Cassidy,Jorge O. Escobedo,Robert M. Strongin
标识
DOI:10.1002/anie.202004094
摘要
Abstract 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 μ 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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