Details of Xenobiotics-DME Interaction (XEOTIC)

General Information of Drug-Metabolizing Enzyme (DME ID: DME0041)
DME Name UDP-glucuronosyltransferase 1A3 (UGT1A3), Homo sapiens DME Info
UniProt ID
UD13_HUMAN
EC Number    EC: 2.4.1.17     (Click to Show/Hide the Complete EC Tree)
Transferase
Glycosyltransferases
Hexosyltransferase
EC: 2.4.1.17
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)
                  Carcinogen Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Methylcholanthrene Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00899   XEOTIC Info Gene Form mRNA
                                 Classification Carcinogen
                                 DME Modulation Methylcholanthrene up-regulates the expression of DME UGT1A3 [1]
                  Environmental Pollutant Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Zinc Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01512   XEOTIC Info Gene Form Protein
                                 Classification Environmental Pollutant
                                 DME Modulation Zinc induces the drug-metabolizing activity of DME UGT1A3 [2]
                  Health Hazard/Toxicant Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Pirinixic acid Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01433   XEOTIC Info Gene Form Protein
                                 Classification Health Hazard
                                 DME Modulation Pirinixic acid induces the drug-metabolizing activity of DME UGT1A3 [3]
      Natural Product(s), Extract(s) or Medicine(s)
                  Natural Product Click to Show/Hide the Full List of Xenobiotics:        2 Xenobiotics
                              Amentoflavone Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01195   XEOTIC Info Gene Form Protein
                                 Classification Natural Product
                                 DME Modulation Amentof DMElavone inhibits the drug-metabolizing activity of DME UGT1A3 [4]
                              Bilirubin Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00877   XEOTIC Info Gene Form Protein
                                 Classification Natural Product
                                 DME Modulation Bilirubin inhibits the drug-metabolizing activity of DME UGT1A3 [5]
      Pharmaceutical Agent(s)
                  Approved/Marketed Drug Click to Show/Hide the Full List of Xenobiotics:        7 Xenobiotics
                              Diclofenac Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00352   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Diclof DMEenac inhibits the drug-metabolizing activity of DME UGT1A3 [5]
                              Estradiol Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00090   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Estradiol inhibits the expression of DME UGT1A3 [6]
                              Fenofibrate Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00035   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Fenofibrate up-regulates the expression of DME UGT1A3 [7]
                              Rifampin Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00223   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Rifampin induces the drug-metabolizing activity of DME UGT1A3 [8], [9]
                              Rosiglitazone Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00380   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Rosiglitazone up-regulates the expression of DME UGT1A3 [10]
                              Warfarin Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00400   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Warfarin up-regulates the expression of DME UGT1A3 [11]
                              Flunitrazepam Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00498   XEOTIC Info Gene Form Protein
                                 Classification Drug Marketed but not Approved by US FDA
                                 DME Modulation Flunitrazepam inhibits the drug-metabolizing activity of DME UGT1A3 [5]
                  Drug in Phase 2 Clinical Trial Click to Show/Hide the Full List of Xenobiotics:        2 Xenobiotics
                              Bisphenol A Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01226   XEOTIC Info Gene Form mRNA
                                 Classification Highest Clinical Status: Phase 2
                                 DME Modulation Bisphenol A inhibits the expression of DME UGT1A3 [6], [12]
                              Genistein Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00557   XEOTIC Info Gene Form mRNA
                                 Classification Highest Clinical Status: Phase 2
                                 DME Modulation Genistein inhibits the expression of DME UGT1A3 [6]
                  Drug in Phase 1 Clinical Trial Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Hymecromone Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00555   XEOTIC Info Gene Form Protein
                                 Classification Highest Clinical Status: Phase 1/2
                                 DME Modulation Hymecromone induces the drug-metabolizing activity of DME UGT1A3 [13]
                  Preclinical/Patented Drug Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              (+)-JQ1 Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00723   XEOTIC Info Gene Form mRNA
                                 Classification Drug in Preclinical Study
                                 DME Modulation (+)-JQ1 inhibits the expression of DME UGT1A3 [14]
                  Investigative Agent Click to Show/Hide the Full List of Xenobiotics:        2 Xenobiotics
                              Beta-naphthoflavone Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01220   XEOTIC Info Gene Form mRNA
                                 Classification Investigative Agent
                                 DME Modulation Beta-naphthoflavone up-regulates the expression of DME UGT1A3 [15], [16]
                              Lithocholic acid Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00787   XEOTIC Info Gene Form mRNA
                                 Classification Investigative Agent
                                 DME Modulation Lithocholic acid up-regulates the expression of DME UGT1A3 [17]
References
1 Keratinocyte gene expression profiles discriminate sensitizing and irritating compounds. Toxicol Sci. 2010 Sep;117(1):81-9.
2 Vitamin D protects against particles-caused lung injury through induction of autophagy in an Nrf2-dependent manner. Environ Toxicol. 2019 May;34(5):594-609.
3 Roles of nitric oxide in inflammatory downregulation of human cytochromes P450. Free Radic Biol Med. 2008 Mar 15;44(6):1161-8.
4 Amentoflavone is a potent broad-spectrum inhibitor of human UDP-glucuronosyltransferases. Chem Biol Interact. 2018 Mar 25;284:48-55.
5 Identification of human UDP-glucuronosyltransferase enzyme(s) responsible for the glucuronidation of 3-hydroxydesloratadine. Biopharm Drug Dispos. 2004 Sep;25(6):243-52.
6 Convergent transcriptional profiles induced by endogenous estrogen and distinct xenoestrogens in breast cancer cells. Carcinogenesis. 2006 Aug;27(8):1567-78.
7 Human UDP-glucuronosyltransferase (UGT)1A3 enzyme conjugates chenodeoxycholic acid in the liver. Hepatology. 2006 Nov;44(5):1158-70.
8 Resveratrol stimulates nitric oxide production by increasing estrogen receptor alpha-Src-caveolin-1 interaction and phosphorylation in human umbilical vein endothelial cells. FASEB J. 2008 Jul;22(7):2185-97.
9 Pro-angiogenic effects of resveratrol in brain endothelial cells: nitric oxide-mediated regulation of vascular endothelial growth factor and metalloproteinases. J Cereb Blood Flow Metab. 2012 May;32(5):884-95.
10 Expression and transcriptional regulation of ABC transporters and cytochromes P450 in hCMEC/D3 human cerebral microvascular endothelial cells. Biochem Pharmacol. 2009 Mar 1;77(5):897-909.
11 A new in vitro method for identifying chemical sensitizers combining peptide binding with ARE/EpRE-mediated gene expression in human skin cells. Cutan Ocul Toxicol. 2010 Sep;29(3):171-92.
12 Bisphenol A-associated alterations in the expression and epigenetic regulation of genes encoding xenobiotic metabolizing enzymes in human fetal liver. Environ Mol Mutagen. 2014 Apr;55(3):184-95.
13 Assessment of the inhibition potential of Licochalcone A against human UDP-glucuronosyltransferases. Food Chem Toxicol. 2016 Apr;90:112-22.
14 CCAT1 is an enhancer-templated RNA that predicts BET sensitivity in colorectal cancer. J Clin Invest. 2016 Feb;126(2):639-52.
15 Use of mRNA expression to detect the induction of drug metabolising enzymes in rat and human hepatocytes. Toxicol Appl Pharmacol. 2009 Feb 15;235(1):86-96.
16 Characterization of xenobiotic metabolizing enzymes of a reconstructed human epidermal model from adult hair follicles. Toxicol Appl Pharmacol. 2017 Aug 15;329:190-201.
17 Cytotoxic and anti-inflammatory effects of onion peel extract on lipopolysaccharide stimulated human colon carcinoma cells. Food Chem Toxicol. 2013 Dec;62:199-204.

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