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Literature summary for 1.17.4.5 extracted from

  • Tie, J.K.; Jin, D.Y.; Tie, K.; Stafford, D.W.
    Evaluation of warfarin resistance using TALENs-mediated vitamin K epoxide reductase knockout HEK293 cells (2013), J. Thromb. Haemost., 11, 1556-1564.
    View publication on PubMedView publication on EuropePMC

Protein Variants

Protein Variants Comment Organism
L128R the naturally occuring mutant shows significantly increased warfarin resistance, but its enzyme activity is 2fold higher compared to wild-type VKOR Homo sapiens
additional information knockout of endogenous VKOR activity, i.e. VKOR and VKORC1L1 enzymes, in HEK-293 cells by transcription activator-like effector nucleases (TALENs)-mediated genome editing, overview Homo sapiens
additional information the W59R mutant has lower activity but higher warfarin resistance than the W59L mutant, warfarin resistance evaluation of the naturally occurring VKOR mutants, overview Homo sapiens
W59L the naturally occuring mutant shows significantly increased warfarin resistance, but its enzyme activity is 2fold higher compared to wild-type VKOR Homo sapiens
W59R the naturally occuring mutant shows significantly increased warfarin resistance, but its enzyme activity is similar to wild-type VKOR Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information evaluation of warfarin resistance using TALENs-mediated vitamin K epoxide reductase knockout HEK293 cells, overview Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2-methyl-3-phytyl-1,4-naphthoquinone + oxidized dithiothreitol + H2O Homo sapiens
-
2,3-epoxy-2,3-dihydro-2-methyl-3-phytyl-1,4-naphthoquinone + 1,4-dithiothreitol
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-methyl-3-phytyl-1,4-naphthoquinone + oxidized dithiothreitol + H2O
-
Homo sapiens 2,3-epoxy-2,3-dihydro-2-methyl-3-phytyl-1,4-naphthoquinone + 1,4-dithiothreitol
-
?

Synonyms

Synonyms Comment Organism
vitamin K epoxide reductase
-
Homo sapiens
VKOR
-
Homo sapiens
VKORC1L1
-
Homo sapiens

General Information

General Information Comment Organism
additional information conserved loop cysteines in VKOR are not required for active site regeneration after each cycle of oxidation. Missense mutations identified in the VKOR coding region, especially hotspot mutation at position 139, lead to a VKOR molecule more resistant to warfarin inhibition, thus requiring higher therapeutic warfarin doses Homo sapiens