Inhibition of thioredoxin reductase by curcumin analogs |
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Authors: | Liu Zhong Du Zhi-Yun Huang Zhi-Shu Lee Kin-Sing Gu Lian-Quan |
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Affiliation: | School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, PR China. |
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Abstract: | Curcumin analogs were first investigated for their inhibitory effects on thioredoxin reductase (TrxR). Most of them were more potent TrxR inhibitors than natural curcumin. The structure-activity relationship was summarized, and the curcumin analog was found to inhibit TrxR irreversibly in a time-dependent manner. The action was caused by covalent modification of the redox-active residues Cys(497) and Sec(498) in TrxR. |
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