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

被引：5
作者：
Koh, Wei Xiang [1 ]
Coppo, Lucia [2 ]
Ganguly, Rakesh [1 ,3 ]
Holmgren, Arne [2 ]
Leong, Weng Kee [1 ]
机构：
[1] Nanyang Technol Univ, Div Chem & Biol Chem, 21 Nanyang Link, Singapore 637371, Singapore
[2] Karolinska Inst, Dept Med Biochem & Biophys, Div Biochem, MBB Biokemi Floor 9A,Solnavagen 9, SE-17165 Stockholm, Sweden
[3] Shiv Nadar Univ, NH91, Greater Noida 201314, Gautam Buddha N, India
来源：
JOURNAL OF ORGANOMETALLIC CHEMISTRY | 2021年 / 943卷
关键词：
Ebselen; Metallocenyl; Thioredoxin reductase; Thioredoxin; Inhibition; Substrate; MAMMALIAN THIOREDOXIN; ACTIVE-SITE; GLUTATHIONE; SYSTEM; GLUTAREDOXIN; MECHANISM; CYSTEINE;
D O I：
10.1016/j.jorganchem.2021.121822
中图分类号：
O61 [无机化学];
学科分类号：
070301 ; 081704 ;
摘要：
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 mu M, 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. (C) 2021 Elsevier B.V. All rights reserved.
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页数：6
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