General Information of Drug-Metabolizing Enzyme (DME ID: DME0149)
DME Name Vitamin K1 2,3-epoxide reductase 1 (VKOR), Homo sapiens DME Info
UniProt ID
VKOR1_HUMAN
EC Number    EC: 1.17.4.4     (Click to Show/Hide the Complete EC Tree)
Oxidoreductase
CH/CH2 oxidoreductase
Disulfide acceptor oxidoreductase
EC: 1.17.4.4
Lineage    Species: Homo sapiens     (Click to Show/Hide the Complete Species Lineage)
Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Primates
Family: Hominidae
Genus: Homo
Species: Homo sapiens
Interactome
Interactions between Xenobiotics and DME (XEOTIC)
      Health or Environmental Toxicant(s)
                  Acute Toxic Substance Click to Show/Hide the Full List of Xenobiotics:        3 Xenobiotics
                              Bromadiolone Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01616   XEOTIC Info Gene Form Protein
                                 Classification Acute Toxic Substance
                                 DME Modulation Bromadiolone inhibits the drug-metabolizing activity of DME VKORC1 [1]
                              Chloropicrin Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01247   XEOTIC Info Gene Form mRNA
                                 Classification Acute Toxic Substance
                                 DME Modulation Chloropicrin up-regulates the expression of DME VKORC1 [2]
                              Coumatetralyl Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01617   XEOTIC Info Gene Form Protein
                                 Classification Acute Toxic Substance
                                 DME Modulation Coumatetralyl inhibits the drug-metabolizing activity of DME VKORC1 [1]
                  Carcinogen Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Benzo(a)pyrene Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00898   XEOTIC Info Gene Form mRNA
                                 Classification Carcinogen
                                 DME Modulation Benzo(a)pyrene inhibits the expression of DME VKORC1 [3]
      Natural Product(s), Extract(s) or Medicine(s)
                  Traditional Medicine Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Jinfukang Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00760   XEOTIC Info Gene Form mRNA
                                 Classification Traditional Medicine
                                 DME Modulation Jinfukang up-regulates the expression of DME VKORC1 [4]
      Pharmaceutical Agent(s)
                  Approved/Marketed Drug Click to Show/Hide the Full List of Xenobiotics:        6 Xenobiotics
                              Copper sulfate Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00117   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Copper sulfate inhibits the expression of DME VKORC1 [5]
                              Cyclosporine Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00241   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Cyclosporine inhibits the expression of DME VKORC1 [3]
                              Doxorubicin hydrochloride Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00292   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Doxorubicin hydrochloride inhibits the expression of DME VKORC1 [6]
                              Phenprocoumon Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00206   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Phenprocoumon inhibits the expression of DME VKORC1 and leads to decreasing the drug-metabolizing activity of this enzyme [7]
                              Acenocoumarol Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00513   XEOTIC Info Gene Form Protein
                                 Classification Drug Marketed but not Approved by US FDA
                                 DME Modulation Acenocoumarol inhibits the drug-metabolizing activity of DME VKORC1 [1]
                              Fluindione Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00471   XEOTIC Info Gene Form Protein
                                 Classification Drug Marketed but not Approved by US FDA
                                 DME Modulation Fluindione inhibits the drug-metabolizing activity of DME VKORC1 [1]
                  Drug in Phase 3 Clinical Trial Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Vitamin E Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00547   XEOTIC Info Gene Form mRNA
                                 Classification Highest Clinical Status: Phase 3
                                 DME Modulation Vitamin E up-regulates the expression of DME VKORC1 [8]
                  Preclinical/Patented Drug Click to Show/Hide the Full List of Xenobiotics:        2 Xenobiotics
                              ICG-001 Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01336   XEOTIC Info Gene Form mRNA
                                 Classification Patented Pharmaceutical Agent
                                 DME Modulation ICG-001 up-regulates the expression of DME VKORC1 [9]
                              K-7174 Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01348   XEOTIC Info Gene Form mRNA
                                 Classification Patented Pharmaceutical Agent
                                 DME Modulation K-7174 inhibits the expression of DME VKORC1 [10]
                  Investigative Agent Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              4-hydroxycoumarin Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00866   XEOTIC Info Gene Form Protein
                                 Classification Investigative Agent
                                 DME Modulation 4-hydroxycoumarin inhibits the drug-metabolizing activity of DME VKORC1 [1]
References
1 VKORC1 and VKORC1L1 have distinctly different oral anticoagulant dose-response characteristics and binding sites. Blood Adv. 2018 Mar 27;2(6):691-702.
2 Transcriptomic analysis of human primary bronchial epithelial cells after chloropicrin treatment. Chem Res Toxicol. 2015 Oct 19;28(10):1926-35.
3 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
4 Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
5 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
6 Bringing in vitro analysis closer to in vivo: studying doxorubicin toxicity and associated mechanisms in 3D human microtissues with PBPK-based dose modelling. Toxicol Lett. 2018 Sep 15;294:184-192.
7 Effects of phenacetin and its metabolite p-phenetidine on COX-1 and COX-2 activities and expression in vitro. Thromb Res. 2003 Jun 15;110(5-6):299-303.
8 Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
9 Altering cancer transcriptomes using epigenomic inhibitors. Epigenetics Chromatin. 2015 Feb 24;8:9.
10 A low-molecular-weight compound K7174 represses hepcidin: possible therapeutic strategy against anemia of chronic disease. PLoS One. 2013 Sep 27;8(9):e75568.

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