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Warfarin and vitamin K epoxide reductase: a molecular accounting for observed inhibition.

Blood. 2018; 
WuSangwook,ChenXuejie,JinDa-Yun,StaffordDarrel W,PedersenLee G,TieJia
Products/Services Used Details Operation
Mouse anti-tubulin monoclonal antibody (Cat# A01410) was from GenScript (Piscataway, NJ).

摘要

Vitamin K epoxide reductase (VKOR), an endoplasmic reticulum membrane protein, is the key enzyme for vitamin K-dependent carboxylation, a posttranslational modification that is essential for the biological functions of coagulation factors. VKOR is the target of the most widely prescribed oral anticoagulant, warfarin. However, the topological structure of VKOR and the mechanism of warfarin's inhibition of VKOR remain elusive. Additionally, it is not clear why warfarin-resistant VKOR mutations identified in patients significantly decrease warfarin's binding affinity, but have only a minor effect on vitamin K binding. Here, we used immunofluorescence confocal imaging of VKOR in live mammalian cells... More

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