Protein Information

ID 1892
Name VKORC1
Synonyms Vitamin K epoxide reductase; IMAGE3455200; MST134; MST576; MSTP134; MSTP576; Phylloquinone epoxide reductase; UNQ308…

Compound Information

ID 1774
Name warfarin
CAS

Reference

PubMed Abstract RScore(About this table)
18374197 Wallin R, Wajih N, Hutson SM: VKORC1: a warfarin-sensitive enzyme in vitamin K metabolism and biosynthesis of vitamin K-dependent blood coagulation factors. Vitam Horm. 2008;78:227-46.
The recently discovered enzyme VKORC1 of the vitamin K cycle, which is the target for the anticoagulant drug warfarin, has opened new opportunities to understand warfarin resistance and biosynthesis of vitamin K-dependent blood coagulation factors and other members of this protein family. Furthermore, it has opened new opportunities to study the vitamin K-dependent posttranslational gamma-carboxylational system in the endoplasmic reticulum in greater detail and its molecular operation in vivo. Other accomplishments resulting from this discovery are: (1) the finding that VKORC1 is the rate-limiting step in biosynthesis of functional vitamin K-dependent proteins, and (2) engineering of recombinant intracellular gamma-carboxylation systems in cell lines producing recombinant coagulation factor used clinically to treat bleeding disorders. The engineered cells significantly enhance production of the fraction of fully functional gamma-carboxylated proteins compared to cell lines only overexpressing the specific coagulation factor. The first described inhibitor of the gamma-carboxylation system has been identified as calumenin, a resident chaperone in the endoplasmic reticulum (ER). Together, the new information gained about the vitamin K-dependent gamma-carboxylation system will stimulate new research which will benefit medicine and our understanding of the molecular mechanisms involved in this protein modification reaction.
63(0,2,2,3)