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Metallocenyl derivatives of ebselen are selective and competitive inhibitors of thioredoxin reductase

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ABSTRACT Ferrocenyl and ruthenocenyl derivatives of ebselen are found to be competitive inhibitors of mammalian TrxR, with IC50 of 4.2 ± 0.3 and 2.5 ± 0.3 µM, respectively. The inhibition… Click to show full abstract

ABSTRACT Ferrocenyl and ruthenocenyl derivatives of ebselen are found to be competitive inhibitors of mammalian TrxR, with IC50 of 4.2 ± 0.3 and 2.5 ± 0.3 µM, respectively. The inhibition of TrxR is selective over GR, and in the presence of excess GSH. They exhibit lower Km values than ebselen and the natural substrate, Trx.

Keywords: competitive inhibitors; derivatives ebselen; ebselen selective; inhibitors thioredoxin; selective competitive; metallocenyl derivatives

Journal Title: Journal of Organometallic Chemistry
Year Published: 2021

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