Inhibition of thioredoxin reductase by curcumin analogs.
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.
Liu
Zhong
Z
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, PR China.
Du
Zhi-Yun
ZY
Huang
Zhi-Shu
ZS
Lee
Kin-Sing
KS
Gu
Lian-Quan
LQ
D003474:Curcumin / Q000031:analogs & derivatives* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D013880:Thioredoxin-Disulfide Reductase / Q000037:antagonists & inhibitors* / Q000378:metabolism
D004791:Enzyme Inhibitors; D013880:Thioredoxin-Disulfide Reductase; D003474:Curcumin