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

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

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 natura...

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Main Authors: Koh, Wei Xiang, Coppo, Lucia, Ganguly, Rakesh, Holmgren, Arne, Leong, Weng Kee
Other Authors: School of Physical and Mathematical Sciences
Format: Article
Language:English
Published: 2022
Subjects:
Science::Chemistry
Ebselen
Metallocenyl
Online Access:https://hdl.handle.net/10356/159768
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Institution: Nanyang Technological University
Language: English
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spelling sg-ntu-dr.10356-1597682022-07-01T07:26:44Z Metallocenyl derivatives of ebselen are selective and competitive inhibitors of thioredoxin reductase Koh, Wei Xiang Coppo, Lucia Ganguly, Rakesh Holmgren, Arne Leong, Weng Kee School of Physical and Mathematical Sciences Science::Chemistry Ebselen Metallocenyl 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. Ministry of Education (MOE) Nanyang Technological University This work was supported by Nanyang Technological University and the Ministry of Education, Singapore (grant no. RG121/18). 2022-07-01T07:26:43Z 2022-07-01T07:26:43Z 2021 Journal Article Koh, W. X., Coppo, L., Ganguly, R., Holmgren, A. & Leong, W. K. (2021). Metallocenyl derivatives of ebselen are selective and competitive inhibitors of thioredoxin reductase. Journal of Organometallic Chemistry, 943, 121822-. https://dx.doi.org/10.1016/j.jorganchem.2021.121822 0022-328X https://hdl.handle.net/10356/159768 10.1016/j.jorganchem.2021.121822 2-s2.0-85105829957 943 121822 en RG121/18 Journal of Organometallic Chemistry © 2021 Elsevier B.V. All rights reserved.
institution Nanyang Technological University
building NTU Library
continent Asia
country Singapore
Singapore
content_provider NTU Library
collection DR-NTU
language English
topic Science::Chemistry
Ebselen
Metallocenyl
spellingShingle Science::Chemistry
Ebselen
Metallocenyl
Koh, Wei Xiang
Coppo, Lucia
Ganguly, Rakesh
Holmgren, Arne
Leong, Weng Kee
Metallocenyl derivatives of ebselen are selective and competitive inhibitors of thioredoxin reductase
description 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.
author2 School of Physical and Mathematical Sciences
author_facet School of Physical and Mathematical Sciences
Koh, Wei Xiang
Coppo, Lucia
Ganguly, Rakesh
Holmgren, Arne
Leong, Weng Kee
format Article
author Koh, Wei Xiang
Coppo, Lucia
Ganguly, Rakesh
Holmgren, Arne
Leong, Weng Kee
author_sort Koh, Wei Xiang
title Metallocenyl derivatives of ebselen are selective and competitive inhibitors of thioredoxin reductase
title_short Metallocenyl derivatives of ebselen are selective and competitive inhibitors of thioredoxin reductase
title_full Metallocenyl derivatives of ebselen are selective and competitive inhibitors of thioredoxin reductase
title_fullStr Metallocenyl derivatives of ebselen are selective and competitive inhibitors of thioredoxin reductase
title_full_unstemmed Metallocenyl derivatives of ebselen are selective and competitive inhibitors of thioredoxin reductase
title_sort metallocenyl derivatives of ebselen are selective and competitive inhibitors of thioredoxin reductase
publishDate 2022
url https://hdl.handle.net/10356/159768
_version_ 1738844947175440384

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