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

Wei Xiang Koh; Lucia Coppo; Rakesh Ganguly; Arne Holmgren; Weng Kee Leong

doi:10.1016/j.jorganchem.2021.121822

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

Wei Xiang Koh, Lucia Coppo, Rakesh Ganguly, Arne Holmgren, Weng Kee Leong^*

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

6 Citations (Scopus)

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.

Original language	English
Article number	121822
Journal	Journal of Organometallic Chemistry
Volume	943
DOIs	https://doi.org/10.1016/j.jorganchem.2021.121822
Publication status	Published - Jun 21 2021
Externally published	Yes

Bibliographical note

Publisher Copyright:
© 2021 Elsevier B.V.

ASJC Scopus Subject Areas

Biochemistry
Physical and Theoretical Chemistry
Organic Chemistry
Inorganic Chemistry
Materials Chemistry

Keywords

Ebselen
Inhibition
Metallocenyl
Substrate
Thioredoxin
Thioredoxin reductase

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10.1016/j.jorganchem.2021.121822

Cite this

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title = "Metallocenyl derivatives of ebselen are selective and competitive inhibitors of thioredoxin reductase",

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 = "Ebselen, Inhibition, Metallocenyl, Substrate, Thioredoxin, Thioredoxin reductase",

author = "Koh, {Wei Xiang} and Lucia Coppo and Rakesh Ganguly and Arne Holmgren and Leong, {Weng Kee}",

note = "Publisher Copyright: {\textcopyright} 2021 Elsevier B.V.",

year = "2021",

month = jun,

day = "21",

doi = "10.1016/j.jorganchem.2021.121822",

language = "English",

volume = "943",

journal = "Journal of Organometallic Chemistry",

issn = "0022-328X",

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TY - JOUR

T1 - Metallocenyl derivatives of ebselen are selective and competitive inhibitors of thioredoxin reductase

AU - Koh, Wei Xiang

AU - Coppo, Lucia

AU - Ganguly, Rakesh

AU - Holmgren, Arne

AU - Leong, Weng Kee

PY - 2021/6/21

Y1 - 2021/6/21

N2 - 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.

AB - 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.

KW - Ebselen

KW - Inhibition

KW - Metallocenyl

KW - Substrate

KW - Thioredoxin

KW - Thioredoxin reductase

UR - http://www.scopus.com/inward/record.url?scp=85105829957&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=85105829957&partnerID=8YFLogxK

U2 - 10.1016/j.jorganchem.2021.121822

DO - 10.1016/j.jorganchem.2021.121822

M3 - Article

AN - SCOPUS:85105829957

SN - 0022-328X

VL - 943

JO - Journal of Organometallic Chemistry

JF - Journal of Organometallic Chemistry

M1 - 121822

ER -

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

Abstract

Bibliographical note

ASJC Scopus Subject Areas

Keywords

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