Details of Xenobiotics-DME Interaction (XEOTIC)

General Information of Drug-Metabolizing Enzyme (DME ID: DME0199)
DME Name Corticosteroid 11-beta-dehydrogenase 1 (HSD11B1), Homo sapiens DME Info
UniProt ID
DHI1_HUMAN
EC Number    EC: 1.1.1.146     (Click to Show/Hide the Complete EC Tree)
Oxidoreductase
CH-OH donor oxidoreductase
NAD/NADP oxidoreductase
EC: 1.1.1.146
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:        2 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 HSD11B1 [1]
                              Aflatoxin B1 Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00806   XEOTIC Info Gene Form mRNA
                                 Classification Carcinogen-mycotoxin
                                 DME Modulation Aflatoxin B1 inhibits the expression of DME HSD11B1 [2], [3]
                  Environmental Pollutant Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              p,p'-Hydroxy-DDT Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01110   XEOTIC Info Gene Form Protein
                                 Classification Environmental Pollutant
                                 DME Modulation p,p'-Hydroxy-DDT inhibits the drug-metabolizing activity of DME HSD11B1 [4]
                  Health Hazard/Toxicant Click to Show/Hide the Full List of Xenobiotics:        2 Xenobiotics
                              Perfluorooctane sulfonic acid Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00921   XEOTIC Info Gene Form Protein
                                 Classification Health and Environmental Toxicant
                                 DME Modulation Perfluorooctane sulfonic acid inhibits the drug-metabolizing activity of DME HSD11B1 [5]
                              Dioctyl adipate Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01613   XEOTIC Info Gene Form Protein
                                 Classification Health Hazard
                                 DME Modulation Dioctyl adipate inhibits the drug-metabolizing activity of DME HSD11B1 [6]
      Natural Product(s), Extract(s) or Medicine(s)
                  Natural Mixture Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Tobacco smoke pollution Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00821   XEOTIC Info Gene Form Protein
                                 Classification Natural Mixture
                                 DME Modulation Tobacco smoke pollution induces the drug-metabolizing activity of DME HSD11B1 [7]
                  Natural Product Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              18alpha-glycyrrhetinic acid Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01098   XEOTIC Info Gene Form Protein
                                 Classification Natural Product
                                 DME Modulation 18alpha-glycyrrhetinic acid inhibits the drug-metabolizing activity of DME HSD11B1 in Human embryonic kidney 293 cell (HEK293) (IC50 = 0.0086 microM) [8]
      Pharmaceutical Agent(s)
                  Approved/Marketed Drug Click to Show/Hide the Full List of Xenobiotics:      19 Xenobiotics
                              Acetaminophen Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00217   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Acetaminophen inhibits the expression of DME HSD11B1 [9]
                              Alitretinoin Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00167   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Alitretinoin inhibits the expression of DME HSD11B1 [10]
                              Azathioprine Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00007   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Azathioprine inhibits the expression of DME HSD11B1 [11]
                              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 HSD11B1 [1]
                              Dexamethasone Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00088   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Dexamethasone up-regulates the expression of DME HSD11B1 and leads to increasing the drug-metabolizing activity of this enzyme [12]
                              Dinoprostone Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00260   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Dinoprostone induces the drug-metabolizing activity of DME HSD11B1 [13]
                              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 HSD11B1 [14]
                              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 HSD11B1 [15]
                              Hydrocortisone Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00264   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Hydrocortisone induces the drug-metabolizing activity of DME HSD11B1 [16], [17]
                              Isotretinoin Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00186   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Isotretinoin inhibits the expression of DME HSD11B1 [18], [10]
                              Metyrapone Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00063   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Metyrapone inhibits the expression of DME HSD11B1 [19]
                              Piroxicam Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00204   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Piroxicam inhibits the drug-metabolizing activity of DME HSD11B1 [20]
                              Progesterone Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00094   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Progesterone up-regulates the expression of DME HSD11B1 [21]
                              Rosiglitazone Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00380   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Rosiglitazone induces the drug-metabolizing activity of DME HSD11B1 [22]
                              Testosterone Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00095   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Testosterone up-regulates the expression of DME HSD11B1 [23]
                              Troglitazone Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00086   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Troglitazone up-regulates the expression of DME HSD11B1 [24]
                              Zoledronic acid Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00140   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Zoledronic acid up-regulates the expression of DME HSD11B1 [25]
                              Carbenoxolone Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01236   XEOTIC Info Gene Form Protein
                                 Classification Drug Marketed but not Approved by US FDA
                                 DME Modulation Carbenoxolone inhibits the drug-metabolizing activity of DME HSD11B1 (IC50 = 0.083 microM) [26]
                              Zinc sulfate Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00460   XEOTIC Info Gene Form Protein
                                 Classification Drug Marketed but not Approved by US FDA
                                 DME Modulation Zinc sulfate inhibits the drug-metabolizing activity of DME HSD11B1 [27]
                  Drug in Phase 2 Clinical Trial Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Bisphenol A Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01226   XEOTIC Info Gene Form Protein
                                 Classification Highest Clinical Status: Phase 2
                                 DME Modulation Bisphenol A inhibits the drug-metabolizing activity of DME HSD11B1 [28]
                  Drug in Phase 1 Clinical Trial Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Gold sodium thiomalate Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00533   XEOTIC Info Gene Form mRNA
                                 Classification Highest Clinical Status: Phase 1
                                 DME Modulation Gold sodium thiomalate inhibits the expression of DME HSD11B1 [11]
                  Preclinical/Patented Drug Click to Show/Hide the Full List of Xenobiotics:        2 Xenobiotics
                              PF-915275 Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00725   XEOTIC Info Gene Form Protein
                                 Classification Drug in Preclinical Study
                                 DME Modulation PF-915275 inhibits the drug-metabolizing activity of DME HSD11B1 (Ki < 0.001 microM) [29]
                              Butaprost Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00734   XEOTIC Info Gene Form Protein
                                 Classification Patented Pharmaceutical Agent
                                 DME Modulation Butaprost induces the drug-metabolizing activity of DME HSD11B1 [13]
References
1 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.
2 Identification of early target genes of aflatoxin B1 in human hepatocytes, inter-individual variability and comparison with other genotoxic compounds. Toxicol Appl Pharmacol. 2012 Jan 15;258(2):176-87.
3 Aflatoxin B1 induces persistent epigenomic effects in primary human hepatocytes associated with hepatocellular carcinoma. Toxicology. 2016 Mar 28;350-352:31-9.
4 Effects of methoxychlor and its metabolite 2,2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane on 11beta-hydroxysteroid dehydrogenase activities in vitro. Toxicol Lett. 2013 Mar 27;218(1):18-23.
5 Metabolic activation of the cooked meat carcinogen 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine in human prostate. Toxicol Sci. 2018 Jun 1;163(2):543-556.
6 Inhibitory effects of some possible endocrine-disrupting chemicals on the isozymes of human 11beta-hydroxysteroid dehydrogenase and expression of their mRNA in gonads and adrenal glands. Environ Sci. 2005;12(4):219-30.
7 Combination of bioanalytical approaches and quantitative proteomics for the elucidation of the toxicity mechanisms associated to TiO2 nanoparticles exposure in human keratinocytes. Food Chem Toxicol. 2019 May;127:197-205.
8 Potent and novel 11beta-HSD1 inhibitors identified from shape and docking based virtual screening. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5739-44.
9 Multiple microRNAs function as self-protective modules in acetaminophen-induced hepatotoxicity in humans. Arch Toxicol. 2018 Feb;92(2):845-858.
10 Retinoic acid and its 4-oxo metabolites are functionally active in human skin cells in vitro. J Invest Dermatol. 2005 Jul;125(1):143-53.
11 Antirheumatic drug response signatures in human chondrocytes: potential molecular targets to stimulate cartilage regeneration. Arthritis Res Ther. 2009;11(1):R15.
12 Reciprocal regulation of 11beta-hydroxysteroid dehydrogenase 1 and glucocorticoid receptor expression by dexamethasone inhibits human coronary artery smooth muscle cell proliferation in vitro. Mol Cell Biochem. 2011 Jan;346(1-2):69-79.
13 PTGER1 and PTGER2 receptors mediate regulation of progesterone synthesis and type 1 11beta-hydroxysteroid dehydrogenase activity by prostaglandin E2 in human granulosa lutein cells. J Endocrinol. 2007 Sep;194(3):595-602.
14 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.
15 Transcriptomic analysis of untreated and drug-treated differentiated HepaRG cells over a 2-week period. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):27-35.
16 Testosterone stimulates adipose tissue 11beta-hydroxysteroid dehydrogenase type 1 expression in a depot-specific manner in children. J Clin Endocrinol Metab. 2010 Jul;95(7):3300-8.
17 Glucocorticoid-activation system mediated glucocorticoid-insulin-like growth factor 1 (GC-IGF1) axis programming alteration of adrenal dysfunction induced by prenatal caffeine exposure. Toxicol Lett. 2019 Mar 1;302:7-17.
18 Temporal changes in gene expression in the skin of patients treated with isotretinoin provide insight into its mechanism of action. Dermatoendocrinol. 2009 May;1(3):177-87.
19 Delineation of the molecular basis for selenium-induced growth arrest in human prostate cancer cells by oligonucleotide array. Cancer Res. 2003 Jan 1;63(1):52-9.
20 Kinetics and mechanism of inhibition of serine esterases by fluorinated aminophosphonates. Chem Biol Interact. 2010 Sep 6;187(1-3):177-84.
21 Identification of new human pregnane X receptor ligands among pesticides using a stable reporter cell system. Toxicol Sci. 2006 Jun;91(2):501-9.
22 Expression and inducibility of cytochrome P450s (CYP1A1, 2B6, 2E1, 3A4) in human cord blood CD34(+) stem cell-derived differentiating neuronal cells. Toxicol Sci. 2012 Oct;129(2):392-410.
23 The azole fungicide tebuconazole affects human CYP1A1 and CYP1A2 expression by an aryl hydrocarbon receptor-dependent pathway. Food Chem Toxicol. 2019 Jan;123:481-491.
24 Methylated pentavalent arsenic metabolites are bifunctional inducers, as they induce cytochrome P450 1A1 and NAD(P)H:quinone oxidoreductase through AhR- and Nrf2-dependent mechanisms. Free Radic Biol Med. 2014 Feb;67:171-87.
25 Histone deacetylase inhibitors induce FPGS mRNA expression and intracellular accumulation of long-chain methotrexate polyglutamates in childhood acute lymphoblastic leukemia: implications for combination therapy. Leukemia. 2010 Mar;24(3):552-62.
26 Arylsulfonamidothiazoles as a new class of potential antidiabetic drugsDiscovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1. J Med Chem. 2002 Aug 29;45(18):3813-5.
27 Antioxidants prevent the RhoA inhibition evoked by crocidolite asbestos in human mesothelial and mesothelioma cells. Am J Respir Cell Mol Biol. 2011 Sep;45(3):625-31.
28 Inhibition of human and rat 11beta-hydroxysteroid dehydrogenases activities by bisphenol A. Toxicol Lett. 2012 Nov 30;215(2):126-30.
29 N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: discovery of PF-915275. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3493-7.

If you find any error in data or bug in web service, please kindly report it to Dr. Yin and Dr. Li.