UGT1A9

Summary

Gene Symbol: UGT1A9
Description: UDP glucuronosyltransferase family 1 member A9
Alias: HLUGP4, LUGP4, UDPGT, UDPGT 1-9, UGT-1I, UGT1-09, UGT1-9, UGT1.9, UGT1A9S, UGT1AI, UGT1I, UDP-glucuronosyltransferase 1-9, UDP glucuronosyltransferase 1 family, polypeptide A9, UDP glycosyltransferase 1 family, polypeptide A9, UDP-glucuronosyltransferase 1 family polypeptide A9s, UDP-glucuronosyltransferase 1-I, UDP-glucuronosyltransferase 1A9
Species: human
Products:     UGT1A9

Top Publications

  1. Ritter J, Crawford J, Owens I. Cloning of two human liver bilirubin UDP-glucuronosyltransferase cDNAs with expression in COS-1 cells. J Biol Chem. 1991;266:1043-7 pubmed
    ..These cDNAs which encode functional bilirubin UDP-glucuronosyltransferases will allow the isolation of an appropriate gene to develop a gene therapy model for patients which have the totally deficient trait. ..
  2. Sanna S, Busonero F, Maschio A, McArdle P, Usala G, Dei M, et al. Common variants in the SLCO1B3 locus are associated with bilirubin levels and unconjugated hyperbilirubinemia. Hum Mol Genet. 2009;18:2711-8 pubmed publisher
    ..Thus, SLC01B3 appears to be involved in the regulation of serum bilirubin levels in healthy individuals and in some bilirubin-related disorders that are only partially explained by other known gene variants. ..
  3. Villeneuve L, Girard H, Fortier L, Gagné J, Guillemette C. Novel functional polymorphisms in the UGT1A7 and UGT1A9 glucuronidating enzymes in Caucasian and African-American subjects and their impact on the metabolism of 7-ethyl-10-hydroxycamptothecin and flavopiridol anticancer drugs. J Pharmacol Exp Ther. 2003;307:117-28 pubmed
    In vitro metabolic studies revealed that along with UDP-glucuronosyltransferase (UGT) 1A1, the hepatic UGT1A9 and the extrahepatic UGT1A7 are involved in the biotransformation of the active and toxic metabolite of irinotecan, 7-ethyl-10-..
  4. Kang T, Kim H, Ju H, Kim J, Jeon Y, Lee H, et al. Genome-wide association of serum bilirubin levels in Korean population. Hum Mol Genet. 2010;19:3672-8 pubmed publisher
    ..Our result supports the idea that there are considerable ethnic differences in genetic association of bilirubin levels between Koreans and European-derived populations. ..
  5. Fujita K, Ando Y, Nagashima F, Yamamoto W, Eodo H, Araki K, et al. Genetic linkage of UGT1A7 and UGT1A9 polymorphisms to UGT1A1*6 is associated with reduced activity for SN-38 in Japanese patients with cancer. Cancer Chemother Pharmacol. 2007;60:515-22 pubmed
    The phenotypic effects of UGT1A7 and UGT1A9 genetic polymorphisms on the in vivo pharmacokinetics of irinotecan were examined. Eighty-four Japanese patients with cancer who received irinotecan-based chemotherapy were enrolled...
  6. Kuypers D, Naesens M, Vermeire S, Vanrenterghem Y. The impact of uridine diphosphate-glucuronosyltransferase 1A9 (UGT1A9) gene promoter region single-nucleotide polymorphisms T-275A and C-2152T on early mycophenolic acid dose-interval exposure in de novo renal allograft recipients. Clin Pharmacol Ther. 2005;78:351-61 pubmed
    ..using human liver microsomes have shown that T--275A and C--2152T single-nucleotide polymorphisms (SNPs) of the UGT1A9 promoter region are associated with higher hepatic expression of UGT1A9 and increased in vitro glucuronidation ..
  7. Han J, Lim H, Shin E, Yoo Y, Park Y, Lee J, et al. Comprehensive analysis of UGT1A polymorphisms predictive for pharmacokinetics and treatment outcome in patients with non-small-cell lung cancer treated with irinotecan and cisplatin. J Clin Oncol. 2006;24:2237-44 pubmed
    To determine whether uridine diphosphate-glucuronosyltransferase 1A1, UGT1A7, and UGT1A9 polymorphisms affect the pharmacokinetics (PK) of irinotecan and treatment outcome of Korean patients with advanced non-small-cell lung cancer (NSCLC)..
  8. Innocenti F, Kroetz D, Schuetz E, Dolan M, Ramirez J, Relling M, et al. Comprehensive pharmacogenetic analysis of irinotecan neutropenia and pharmacokinetics. J Clin Oncol. 2009;27:2604-14 pubmed publisher
    ..On the basis of this exploratory analysis, common polymorphisms in genes encoding for ABC and SLC transporters may have a significant impact on the pharmacokinetics and pharmacodynamics of CPT-11. Confirmatory studies are required. ..
  9. Tukey R, Strassburg C. Human UDP-glucuronosyltransferases: metabolism, expression, and disease. Annu Rev Pharmacol Toxicol. 2000;40:581-616 pubmed
    ..The role of the UGTs in metabolism and different disease states in humans is the topic of this review. ..

More Information

Publications121 found, 100 shown here

  1. van Es H, Bout A, Liu J, Anderson L, Duncan A, Bosma P, et al. Assignment of the human UDP glucuronosyltransferase gene (UGT1A1) to chromosome region 2q37. Cytogenet Cell Genet. 1993;63:114-6 pubmed
    ..In the present study, we used the cDNA of UGT1A1*4, a bilirubin-conjugating isoform, to localize the UGT1A1 locus in the human genome. The UGT1A1 gene was assigned by in situ hybridization to chromosome region 2q37. ..
  2. Johnson A, Kavousi M, Smith A, Chen M, Dehghan A, Aspelund T, et al. Genome-wide association meta-analysis for total serum bilirubin levels. Hum Mol Genet. 2009;18:2700-10 pubmed publisher
    ..In analyses for association with gallbladder disease or gallstones, top bilirubin SNPs in UGT1A1 and SLCO1B1 were not associated. ..
  3. Carlini L, Meropol N, Bever J, Andria M, Hill T, Gold P, et al. UGT1A7 and UGT1A9 polymorphisms predict response and toxicity in colorectal cancer patients treated with capecitabine/irinotecan. Clin Cancer Res. 2005;11:1226-36 pubmed
    ..013) and lack of severe gastrointestinal toxicity (p = 0.003). In addition, the UGT1A9 -118 (dT)(9/9) genotype was significantly associated with reduced toxicity (p = 0...
  4. Cecchin E, Innocenti F, D Andrea M, Corona G, De Mattia E, Biason P, et al. Predictive role of the UGT1A1, UGT1A7, and UGT1A9 genetic variants and their haplotypes on the outcome of metastatic colorectal cancer patients treated with fluorouracil, leucovorin, and irinotecan. J Clin Oncol. 2009;27:2457-65 pubmed publisher
    ..In addition to UGT1A1*28, UGT1A1*60, UGT1A1*93, UGT1A7*3, and UGT1A9*22 were genotyped in 250 metastatic colorectal cancer patients, and associations with severe hematologic and ..
  5. Vogel A, Kneip S, Barut A, Ehmer U, Tukey R, Manns M, et al. Genetic link of hepatocellular carcinoma with polymorphisms of the UDP-glucuronosyltransferase UGT1A7 gene. Gastroenterology. 2001;121:1136-44 pubmed
    ..This study examines the association of UGT1A7 and UGT1A9 gene polymorphisms with hepatocellular carcinoma...
  6. Yamanaka H, Nakajima M, Katoh M, Hara Y, Tachibana O, Yamashita J, et al. A novel polymorphism in the promoter region of human UGT1A9 gene (UGT1A9*22) and its effects on the transcriptional activity. Pharmacogenetics. 2004;14:329-32 pubmed
    The human UDP-glucuronosyltransferase, UGT1A9, catalyses glucuronidations of various endobiotics and xenobiotics...
  7. Quesnot N, Bucher S, Gade C, Vlach M, Vene E, Valença S, et al. Production of chlorzoxazone glucuronides via cytochrome P4502E1 dependent and independent pathways in human hepatocytes. Arch Toxicol. 2018;92:3077-3091 pubmed publisher
    ..demonstrate that UGT1A1, 1A6 and 1A9 proteins catalyze the synthesis of CHZ-O-Glc while CHZ-N-Glc is produced by UGT1A9 specifically...
  8. Gufford B, Lu J, Metzger I, Jones D, Desta Z. Stereoselective Glucuronidation of Bupropion Metabolites In Vitro and In Vivo. Drug Metab Dispos. 2016;44:544-53 pubmed publisher
    ..formation of glucuronides of hydroxybupropion, (S,S)-hydrobupropion, (S,R)- and (R,S)-hydrobupropion; UGT1A9 catalyzed the formation of (R,R)-hydrobupropion glucuronide...
  9. Kim J, Hwang D, Moon J, Lee Y, Yoo J, Shin D, et al. Multiple UDP-Glucuronosyltransferase and Sulfotransferase Enzymes are Responsible for the Metabolism of Verproside in Human Liver Preparations. Molecules. 2017;22: pubmed publisher
    ..glucuronide (M7), and picroside II glucuronide (M6) was catalyzed by commonly expressed UGT1A1 and UGT1A9 and gastrointestinal-specific UGT1A7, UGT1A8, and UGT1A10, consistent with the higher intrinsic clearance values ..
  10. Lee J, Ha S, Cho E, Choi I. Resveratrol as a Bioenhancer to Improve Anti-Inflammatory Activities of Apigenin. Nutrients. 2015;7:9650-61 pubmed publisher
    ..UGTs), was investigated, resveratrol mainly inhibited the formation of apigenin glucuronides by UGT1A9 in a non-competitive manner with a Ki value of 7.782 μM...
  11. Kwon S, Kim J, Jeong H, Cho Y, Oh S, Lee H. Inhibitory Effects of Aschantin on Cytochrome P450 and Uridine 5'-diphospho-glucuronosyltransferase Enzyme Activities in Human Liver Microsomes. Molecules. 2016;21: pubmed publisher
    ..weakly inhibited UGT1A1-catalyzed SN-38 glucuronidation, UGT1A6-catalyzed N-acetylserotonin glucuronidation, and UGT1A9-catalyzed mycophenolic acid glucuronidation, with IC50 values of 131.7, 144.1, and 71...
  12. Uno Y, Takahira R, Murayama N, Ishii Y, Ikenaka Y, Ishizuka M, et al. Molecular and functional characterization of UDP-glucuronosyltransferase 1A in cynomolgus macaques. Biochem Pharmacol. 2018;155:172-181 pubmed publisher
    ..Among these 11 cynomolgus UGT1A mRNAs, cynomolgus UGT1A2, UGT1A9, and UGT1A10 mRNAs were most abundantly expressed in the liver, kidney, and jejunum, respectively...
  13. Kim J, Kwon S, Kong T, Cheong J, Kim H, In M, et al. AM-2201 Inhibits Multiple Cytochrome P450 and Uridine 5'-Diphospho-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes. Molecules. 2017;22: pubmed publisher
    ..1 μM. It negligibly inhibited CYP1A2, CYP2A6, CYP2B6, CYP2C19, CYP2D6, UGT1A1, UGT1A4, UGT1A6, and UGT1A9 activities at 50 μM in human liver microsomes...
  14. González Mira A, Varo I, Sole M, Torreblanca A. Drugs of environmental concern modify Solea senegalensis physiology and biochemistry in a temperature-dependent manner. Environ Sci Pollut Res Int. 2016;23:20937-20951 pubmed
    ..BFCOD)) and uridine diphosphate glucuronosyltransferase (UDPGT)...
  15. He Y, Folkerts E, Zhang Y, Martin J, Alessi D, Goss G. Effects on Biotransformation, Oxidative Stress, and Endocrine Disruption in Rainbow Trout (Oncorhynchus mykiss) Exposed to Hydraulic Fracturing Flowback and Produced Water. Environ Sci Technol. 2017;51:940-947 pubmed publisher
    ..The increased expression of cyp1a (2.49 ± 0.28-fold), udpgt (2.01 ± 0.31-fold), sod (1.67 ± 0.09-fold), and gpx (1.58 ± 0.10-fold) in raw sample exposure group (7...
  16. Collier A, Yamauchi Y, Sato B, Rougée L, Ward M. UDP-glucuronosyltransferase 1a enzymes are present and active in the mouse blastocyst. Drug Metab Dispos. 2014;42:1921-5 pubmed publisher
    ..Western blots demonstrated the presence of Ugt1a6 but not Ugt1a1, Ugt1a3, Ugt1a4, or Ugt1a9. The Ugt2b proteins were not detected by either assay...
  17. Rouleau M, Audet Delage Y, Desjardins S, Rouleau M, Girard Bock C, Guillemette C. Endogenous Protein Interactome of Human UDP-Glucuronosyltransferases Exposed by Untargeted Proteomics. Front Pharmacol. 2017;8:23 pubmed publisher
    ..An enhanced accumulation of lipid droplets in a kidney cell model overexpressing the UGT1A9 enzyme supported the presence of a functional interplay...
  18. Kong T, Kim J, Kwon S, Cheong J, Kim H, In M, et al. Inhibition of cytochrome P450 and uridine 5'-diphospho-glucuronosyltransferases by MAM-2201 in human liver microsomes. Arch Pharm Res. 2017;40:727-735 pubmed publisher
    ..MAM-2201 (50 µM) negligibly inhibited CYP1A2, CYP2A6, CYP2B6, CYP2C19, CYP2D6, UGT1A1, UGT1A4, UGT1A6, UGT1A9, and UGT2B7...
  19. Benton M, Lea R, Macartney Coxson D, Bellis C, Carless M, Curran J, et al. Serum bilirubin concentration is modified by UGT1A1 haplotypes and influences risk of type-2 diabetes in the Norfolk Island genetic isolate. BMC Genet. 2015;16:136 pubmed publisher
    ..GWAS of blood-based clinical traits in the Norfolk Island population has identified variants within the UDPGT family directly associated with serum bilirubin levels, which is in turn implicated with reduced risk of ..
  20. Richter L, Kaminski Y, Noor F, Meyer M, Maurer H. Metabolic fate of desomorphine elucidated using rat urine, pooled human liver preparations, and human hepatocyte cultures as well as its detectability using standard urine screening approaches. Anal Bioanal Chem. 2016;408:6283-94 pubmed publisher
    ..UDP-glucuronyltransferase (UGT) initial activity screening showed that UGT1A1, UGT1A8, UGT1A9, UGT1A10, UGT2B4, UGT2B7, UGT2B15, and UGT2B17 formed desomorphine glucuronide...
  21. Cengiz B, Yumrutas O, Bozgeyik E, Borazan E, Igci Y, Bozgeyik I, et al. Differential expression of the UGT1A family of genes in stomach cancer tissues. Tumour Biol. 2015;36:5831-7 pubmed publisher
    ..Accordingly, UGT1A1, UGT1A8, and UGT1A10 were found to be upregulated, and UGT1A3, UGT1A5, UGT1A7, and UGT1A9 were downregulated in stomach tumors. No expression changes were observed in UGT1A4...
  22. James A, Blumenstein L, Glaenzel U, Jin Y, Demailly A, Jakab A, et al. Absorption, distribution, metabolism, and excretion of [(14)C]BYL719 (alpelisib) in healthy male volunteers. Cancer Chemother Pharmacol. 2015;76:751-60 pubmed publisher
    ..showed that spontaneous and enzymatic hydrolysis contributed to M4 formation, while CYP3A4-mediated oxidation and UGT1A9-mediated glucuronidation formed minor metabolites...
  23. Yan T, Gao S, Peng X, Shi J, Xie C, Li Q, et al. Significantly decreased and more variable expression of major CYPs and UGTs in liver microsomes prepared from HBV-positive human hepatocellular carcinoma and matched pericarcinomatous tissues determined using an isotope label-free UPLC-MS/MS method. Pharm Res. 2015;32:1141-57 pubmed publisher
    ..05), whereas UGT1A6 and UGT1A9 levels were unchanged (p > 0.05)...
  24. Algeelani S, Alkhelb D, Greenblatt D. Inhibitory effects of sulfonylureas and non-steroidal anti-inflammatory drugs on in vitro metabolism of canagliflozin in human liver microsomes. Biopharm Drug Dispos. 2018;39:135-142 pubmed publisher
    ..against M5 formation, but had relatively selective inhibitory potency against M7 formation, which is catalysed by UGT1A9, with an IC50 value of 1.9 μm and an inhibition constant value of 0.8 μm...
  25. Weiss J, Becker J, Haefeli W. Telaprevir is a substrate and moderate inhibitor of P-glycoprotein, a strong inductor of ABCG2, but not an activator of PXR in vitro. Int J Antimicrob Agents. 2014;43:184-8 pubmed publisher
    ..In contrast, telaprevir had no significant influence on mRNA expression of CYP3A4, UGT1A9, ABCB1, ABCC2 and SLCO1B1. In a reporter gene assay, telaprevir did not activate PXR...
  26. Zhong S, Han W, Hou C, Liu J, Wu L, Liu M, et al. Relation of Transcriptional Factors to the Expression and Activity of Cytochrome P450 and UDP-Glucuronosyltransferases 1A in Human Liver: Co-Expression Network Analysis. AAPS J. 2017;19:203-214 pubmed publisher
    ..TFs (TEAD4, NFKB2, and NFKB1) were negatively associated with mRNA expression of CYP2C9/CYP2E1/UGT1A9. Furthermore, the effect of NR1I2, NR1I3, AR, TEAD4, and NFKB2 on CYP450/UGT1A gene transcription translated into ..
  27. Miners J, Chau N, Rowland A, Burns K, McKinnon R, Mackenzie P, et al. Inhibition of human UDP-glucuronosyltransferase enzymes by lapatinib, pazopanib, regorafenib and sorafenib: Implications for hyperbilirubinemia. Biochem Pharmacol. 2017;129:85-95 pubmed publisher
    ..REG and SOR were equipotent inhibitors of human liver microsomal UGT1A9 (mean Ki 678nM). REG and SOR are the most potent inhibitors of a human UGT enzyme identified to date...
  28. Zeng J, Fan Y, Tan B, Su H, Li Y, Zhang L, et al. Charactering the metabolism of cryptotanshinone by human P450 enzymes and uridine diphosphate glucuronosyltransferases in vitro. Acta Pharmacol Sin. 2018;39:1393-1404 pubmed publisher
    ..This study showed that the metabolites at m/z of 473 were mediated by UGT1A9 and that the metabolites at m/z of 489 were mediated by UGT2B7 and UGT2B4...
  29. Hoydal K, Jenssen B, Letcher R, Dam M, Arukwe A. Hepatic phase I and II biotransformation responses and contaminant exposure in long-finned pilot whales from the Northeastern Atlantic. Mar Environ Res. 2018;134:44-54 pubmed publisher
    ..The activity levels of phase II conjugating enzymes (uridine 5'-diphospho-glucuronosyltransferase [UDPGT], and glutathione S-transferase [GST]) were low...
  30. Cho P, Paudel S, Lee D, Jin Y, Jo G, Jeong T, et al. Characterization of CYPs and UGTs Involved in Human Liver Microsomal Metabolism of Osthenol. Pharmaceutics. 2018;10: pubmed publisher
    ..metabolites (M1-M5) by CYP2D6, 1A2, and 3A4, respectively, a 7-O-glucuronide conjugate (M6) by UGT1A9, and a hydroxyl-glucuronide (M7) from M5 by UGT1A3 in HLMs...
  31. Weiss J, Gajek T, Köhler B, Haefeli W. Venetoclax (ABT-199) Might Act as a Perpetrator in Pharmacokinetic Drug-Drug Interactions. Pharmaceutics. 2016;8: pubmed publisher
    ..Venetoclax induced the mRNA expression of CYP1A1, CYP1A2, UGT1A3, and UGT1A9. In contrast, expression of ABCB1 was suppressed, which might revert tumor resistance towards antineoplastic P-gp ..
  32. Yuan L, Gao Z, Sun H, Qian S, Xiao Y, Sun L, et al. Inter-isoform Hetero-dimerization of Human UDP-Glucuronosyltransferases (UGTs) 1A1, 1A9, and 2B7 and Impacts on Glucuronidation Activity. Sci Rep. 2016;6:34450 pubmed publisher
    ..Moreover, protein interactions also changed the regioselectivity of UGT1A9 for querectin glucuronidation...
  33. Yonekura H, Murayama N, Yamazaki H, Sobue K. A Case of Delayed Emergence After Propofol Anesthesia: Genetic Analysis. A A Case Rep. 2016;7:243-246 pubmed
    ..genetic polymorphisms of cytochrome P450 2B6 (CYP2B6) and uridine 5'-diphospho-glucuronosyltransferase 1A9 (UGT1A9)...
  34. Bins S, Lenting A, El Bouazzaoui S, van Doorn L, Oomen de Hoop E, Eskens F, et al. Polymorphisms in SLCO1B1 and UGT1A1 are associated with sorafenib-induced toxicity. Pharmacogenomics. 2016;17:1483-90 pubmed publisher
    ..with sorafenib at the Erasmus MC Cancer Institute, the Netherlands, for SLCO1B1, SLCO1B3, ABCC2, ABCG2, UGT1A1 and UGT1A9. The UGT1A1 (rs8175347) polymorphism was associated with hyperbilirubinemia and treatment interruption...
  35. Lv X, Zhang J, Wang X, Hu W, Shi Y, Liu S, et al. Amentoflavone is a potent broad-spectrum inhibitor of human UDP-glucuronosyltransferases. Chem Biol Interact. 2018;284:48-55 pubmed publisher
    ..TFP-N-glucuronidation in both UGT1A4 and human liver microsomes, while functioned as a competitive inhibitor of UGT1A9 mediated propofol or 4-MU-O-glucuronidation...
  36. Sandanaraj E, Jada S, Shu X, Lim R, Lee S, Zhou Q, et al. Influence of UGT1A9 intronic I399C>T polymorphism on SN-38 glucuronidation in Asian cancer patients. Pharmacogenomics J. 2008;8:174-85 pubmed
    Genetic polymorphisms in hepatically expressed UGT1A1 and UGT1A9 contribute to the interindividual variability i-n irinotecan disposition and toxicity. We screened UGT1A1 (UGT1A1*60, g.-3140G>A, UGT1A1*28 and UGT1A1*6) and UGT1A9 (g...
  37. Pazik J, Ołdak M, Lewandowski Z, Dąbrowski M, Podgórska M, Sitarek E, et al. Recipient uridine 5'-diphospho-glucuronosyltransferase UGT1A9 c.98T>C variant determines transplanted kidney filtration rate. Transplant Proc. 2014;46:2678-82 pubmed publisher
    ..The medication is metabolized by uridine diphosphate glucuronosyltransferases, mainly UGT1A9 present in liver, kidney, and intestine...
  38. Ehmer U, Vogel A, Schütte J, Krone B, Manns M, Strassburg C. Variation of hepatic glucuronidation: Novel functional polymorphisms of the UDP-glucuronosyltransferase UGT1A4. Hepatology. 2004;39:970-7 pubmed
    ..subjects (128 patients with HCC, 235 blood donors) was analyzed for polymorphisms of the UGT1A3, UGT1A4, UGT1A8, UGT1A9, UGT1A10 genes using polymerase chain reaction, sequencing analysis...
  39. Manevski N, Moreolo P, Yli Kauhaluoma J, Finel M. Bovine serum albumin decreases Km values of human UDP-glucuronosyltransferases 1A9 and 2B7 and increases Vmax values of UGT1A9. Drug Metab Dispos. 2011;39:2117-29 pubmed publisher
    The human UDP-glucuronosyltransferase (UGT) enzymes UGT1A9 and UGT2B7 play important roles in the hepatic glucuronidation of many drugs...
  40. Shiraga T, Yajima K, Suzuki K, Suzuki K, Hashimoto T, Iwatsubo T, et al. Identification of UDP-glucuronosyltransferases responsible for the glucuronidation of darexaban, an oral factor Xa inhibitor, in human liver and intestine. Drug Metab Dispos. 2012;40:276-82 pubmed publisher
    ..3 ?M. Among recombinant human UGTs, UGT1A9 showed the highest intrinsic clearance for darexaban glucuronidation, followed by UGT1A8, -1A10, and -1A7...
  41. Jiamboonsri P, Pithayanukul P, Bavovada R, Leanpolchareanchai J, Gao S, Hu M. In vitro glucuronidation of methyl gallate and pentagalloyl glucopyranose by liver microsomes. Drug Metab Pharmacokinet. 2016;31:292-303 pubmed publisher
    ..For PGG, a mono-glucuronided metabolite was mediated by liver microsomes or UGT1A9. However, a PGG glucuronide was absent in the UGT1A1 system...
  42. Stegeman B, Vos H, Helmerhorst F, Rosendaal F, Reitsma P, van Hylckama Vlieg A. Genetic variation in the first-pass metabolism of ethinylestradiol, sex hormone binding globulin levels and venous thrombosis risk. Eur J Intern Med. 2017;42:54-60 pubmed publisher
    ..SNPs were selected in 11 candidate genes; COMT, CYP1A2, CYP2C9, CYP3A4, CYP3A5, SULT1A1, SULT1E1, UGT1A1, UGT1A3, UGT1A9, UGT2B7. Venous thrombosis risk was expressed as odds ratios (OR) with 95% confidence intervals (CI)...
  43. Zhao W, Fakhoury M, Deschenes G, Roussey G, Brochard K, Niaudet P, et al. Population pharmacokinetics and pharmacogenetics of mycophenolic acid following administration of mycophenolate mofetil in de novo pediatric renal-transplant patients. J Clin Pharmacol. 2010;50:1280-91 pubmed publisher
    ..Body weight, concomitant medication, and UGT2B7 genotype contribute significantly to the interindividual variability of MMF disposition in pediatric renal-transplant patients. ..
  44. Ruiz J, Herrero M, Bosó V, Megías J, Hervás D, Poveda J, et al. Impact of Single Nucleotide Polymorphisms (SNPs) on Immunosuppressive Therapy in Lung Transplantation. Int J Mol Sci. 2015;16:20168-82 pubmed publisher
    ..in other kinds of solid organ transplantation, namely ABCB1 and CYP3A5 genes with tacrolimus (Tac) and ABCC2, UGT1A9 and SLCO1B1 genes with mycophenolic acid (MPA), during the first six months after lung transplantation (51 ..
  45. Cao Y, Du Z, Zhu Z, Sun H, Fu Z, Yang K, et al. Inhibitory effects of fifteen phthalate esters in human cDNA-expressed UDP-glucuronosyltransferase supersomes. Chemosphere. 2017;185:983-990 pubmed publisher
    ..However, UGT1A9 was strongly inhibited by PAEs...
  46. Yamamoto K, Soeda Y, Kamisako T, Hosaka H, Fukano M, Sato H, et al. Analysis of bilirubin uridine 5'-diphosphate (UDP)-glucuronosyltransferase gene mutations in seven patients with Crigler-Najjar syndrome type II. J Hum Genet. 1998;43:111-4 pubmed
    ..Although the first and the second type of mutations are recessive, the third type appears to be dominant with incomplete penetrance, since the allele frequency of the insertion mutation of the TATAA element is very high (40%). ..
  47. Barbier O, Villeneuve L, Bocher V, Fontaine C, Torra I, Duhem C, et al. The UDP-glucuronosyltransferase 1A9 enzyme is a peroxisome proliferator-activated receptor alpha and gamma target gene. J Biol Chem. 2003;278:13975-83 pubmed
    ..Among the UGT1A family enzymes, UGT1A9 metabolizes endogenous compounds, including catecholestrogens, and xenobiotics, such as fibrates and to a lesser ..
  48. Operaña T, Tukey R. Oligomerization of the UDP-glucuronosyltransferase 1A proteins: homo- and heterodimerization analysis by fluorescence resonance energy transfer and co-immunoprecipitation. J Biol Chem. 2007;282:4821-9 pubmed
    ..This technique demonstrated that UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A7, UGT1A8, UGT1A9, and UGT1A10 self-oligomerize (homodimerize)...
  49. Wu B, Wang X, Zhang S, Hu M. Accurate prediction of glucuronidation of structurally diverse phenolics by human UGT1A9 using combined experimental and in silico approaches. Pharm Res. 2012;29:1544-61 pubmed publisher
    Catalytic selectivity of human UGT1A9, an important membrane-bound enzyme catalyzing glucuronidation of xenobiotics, was determined experimentally using 145 phenolics and analyzed by 3D-QSAR methods...
  50. Li X, Yu Y, Zhu G, Qian Y. Cloning of UGT1A9 cDNA from liver tissues and its expression in CHL cells. World J Gastroenterol. 2001;7:841-5 pubmed
    To clone the cDNA of UGT1A9 from a Chinese human liver and establish the Chinese hamster lung (CHL) cell line expressing human UGT1A9...
  51. Johnson L, Oetting W, Basu S, Prausa S, Matas A, Jacobson P. Pharmacogenetic effect of the UGT polymorphisms on mycophenolate is modified by calcineurin inhibitors. Eur J Clin Pharmacol. 2008;64:1047-56 pubmed publisher
    ..We hypothesized that polymorphisms of UGT1A9 and 1A8 may alter MPA pharmacokinetics in kidney transplantation...
  52. Nishiyama T, Fujishima M, Masuda Y, Izawa T, Ohnuma T, Ogura K, et al. Amino acid positions 69-132 of UGT1A9 are involved in the C-glucuronidation of phenylbutazone. Arch Biochem Biophys. 2008;478:75-80 pubmed publisher
    ..Recently, we reported that PB C-glucuronide formation is catalyzed by UGT1A9. Interestingly, despite UGT1A8 sharing high amino acid sequence identity with UGT1A9, UGT1A8 had no PB C-..
  53. Nakajima M, Koga T, Sakai H, Yamanaka H, Fujiwara R, Yokoi T. N-Glycosylation plays a role in protein folding of human UGT1A9. Biochem Pharmacol. 2010;79:1165-72 pubmed publisher
    ..In the present study, we investigated the role of N-glycosylation in the function of human UGT1A9. Mutation analysis at the potential N-glycosylation sites at residues 71, 292, and 344 (from asparagine to ..
  54. Pattanawongsa A, Chau N, Rowland A, Miners J. Inhibition of Human UDP-Glucuronosyltransferase Enzymes by Canagliflozin and Dapagliflozin: Implications for Drug-Drug Interactions. Drug Metab Dispos. 2015;43:1468-76 pubmed publisher
    ..CNF inhibited all UGT1A subfamily enzymes, but the greatest inhibition was observed with UGT1A1, UGT1A9, and UGT1A10 (IC50 values ≤ 10 µM)...
  55. Ohnishi A, Emi Y. Rapid proteasomal degradation of translocation-deficient UDP-glucuronosyltransferase 1A1 proteins in patients with Crigler-Najjar type II. Biochem Biophys Res Commun. 2003;310:735-41 pubmed
    ..8h for WT/1A1. Our findings demonstrate that L15R/1A1 was rapidly degraded by the proteasome owing to its mislocalization in the cell. ..
  56. Ciotti M, Chen F, Rubaltelli F, Owens I. Coding defect and a TATA box mutation at the bilirubin UDP-glucuronosyltransferase gene cause Crigler-Najjar type I disease. Biochim Biophys Acta. 1998;1407:40-50 pubmed
    ..e. paired with itself, as previously reported in the literature, it is far less repressive and generates the mild Gilbert's phenotype. ..
  57. Albert C, Vall e M, Beaudry G, B langer A, Hum D. The monkey and human uridine diphosphate-glucuronosyltransferase UGT1A9, expressed in steroid target tissues, are estrogen-conjugating enzymes. Endocrinology. 1999;140:3292-302 pubmed publisher
    ..The predicted primary structure is most homologous to the human UGT1A9 (hUGT1A9) enzyme, which share 93% identity...
  58. Levesque E, Delage R, Benoit Biancamano M, Caron P, Bernard O, Couture F, et al. The impact of UGT1A8, UGT1A9, and UGT2B7 genetic polymorphisms on the pharmacokinetic profile of mycophenolic acid after a single oral dose in healthy volunteers. Clin Pharmacol Ther. 2007;81:392-400 pubmed
    We studied whether polymorphisms in the UGT1A8, UGT1A9, and UGT2B7 genes, the enzymes producing the phenolic (MPAG) and acyl (AcMPAG) glucuronides of mycophenolic acid (MPA), could contribute to the interindividual variation observed in ..
  59. Kanaya A, Sato T, Fuse N, Yamaguchi H, Mano N, Yamauchi M. Impact of clinical factors and UGT1A9 and CYP2B6 genotype on inter-individual differences in propofol pharmacokinetics. J Anesth. 2018;32:236-243 pubmed publisher
    ..studies in which the association between several potential covariates, including genetic factors such as the UGT1A9 and CYP2B6 genotypes, and propofol pharmacokinetics was simultaneously examined...
  60. Paoluzzi L, Singh A, Price D, Danesi R, Mathijssen R, Verweij J, et al. Influence of genetic variants in UGT1A1 and UGT1A9 on the in vivo glucuronidation of SN-38. J Clin Pharmacol. 2004;44:854-60 pubmed
    ..Recently, several variants in the UGT1A1 and UGT1A9 genes have been described with altered functionality in vitro...
  61. Han J, Lim H, Park Y, Lee S, Lee J. Integrated pharmacogenetic prediction of irinotecan pharmacokinetics and toxicity in patients with advanced non-small cell lung cancer. Lung Cancer. 2009;63:115-20 pubmed publisher
    ..of 107 NSCLC patients treated with irinotecan were evaluated for PK and genotyped for the UGT1A1*6, UGT1A1*28, UGT1A9*22, ABCB11236C>T, 2677G>T/A, 3435C>T, ABCC2-24C>T, 1249G>A, 3972C>T, ABCG234G>A, 421C>A, ..
  62. Menard V, Girard H, Harvey M, Perusse L, Guillemette C. Analysis of inherited genetic variations at the UGT1 locus in the French-Canadian population. Hum Mutat. 2009;30:677-87 pubmed publisher
    ..Four haplotype blocks were inferred: Block 9/6 (UGT1A9, UGT1A7 and UGT1A6), Block 4 (UGT1A4), Block 3/1 (UGT1A3 and UGT1A1), and Block C (3'UTR)...
  63. Manevski N, Kurkela M, Höglund C, Mauriala T, Court M, Yli Kauhaluoma J, et al. Glucuronidation of psilocin and 4-hydroxyindole by the human UDP-glucuronosyltransferases. Drug Metab Dispos. 2010;38:386-95 pubmed publisher
    ..8 mM; V(max) = 2.5 nmol/min/mg). The kinetics of psilocin glucuronidation by UGT1A9 was more complex and may be best described by biphasic kinetics with both intermediate (K(m1) = 1...
  64. Thijs J, Van Der Geest B, van der Schaft J, Van Den Broek M, Van Seggelen W, Bruijnzeel Koomen C, et al. Predicting therapy response to mycophenolic acid using UGT1A9 genotyping: towards personalized medicine in atopic dermatitis. J Dermatolog Treat. 2017;28:242-245 pubmed publisher
    ..Low MPA exposure and increased enzyme activity correlates with the presence of UGT1A9 polymorphisms...
  65. Zheng Y, Min J, Kim D, Park J, Choi S, Lee E, et al. In Vitro Inhibition of Human UDP-Glucuronosyl-Transferase (UGT) Isoforms by Astaxanthin, β-Cryptoxanthin, Canthaxanthin, Lutein, and Zeaxanthin: Prediction of in Vivo Dietary Supplement-Drug Interactions. Molecules. 2016;21: pubmed publisher
    ..inhibitory potential of these xanthophylls on the seven major human hepatic UGTs (UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, UGT2B7 and UGT2B15) in vitro by LC-MS/MS using specific marker reactions in human liver microsomes (except ..
  66. Bosma P, Chowdhury J, Huang T, Lahiri P, Elferink R, van Es H, et al. Mechanisms of inherited deficiencies of multiple UDP-glucuronosyltransferase isoforms in two patients with Crigler-Najjar syndrome, type I. FASEB J. 1992;6:2859-63 pubmed
    ..Presence of identical abnormalities in the common regions of the three mRNAs is consistent with the finding that the common 3' regions of the two B-UGT mRNAs and the P-UGT mRNA are encoded by four shared exons. ..
  67. Yamanaka H, Nakajima M, Hara Y, Katoh M, Tachibana O, Yamashita J, et al. Urinary excretion of phenytoin metabolites, 5-(4'-hydroxyphenyl)-5-phenylhydantoin and its O-glucuronide in humans and analysis of genetic polymorphisms of UDP-glucuronosyltransferases. Drug Metab Pharmacokinet. 2005;20:135-43 pubmed
    ..of 4'-HPPH is catalyzed by multiple UDP-glucuronosyltransferases (UGTs) of UGT1A1, UGT1A4, UGT1A6, and UGT1A9. Since 4'-HPPH may be bioactivated to a reactive metabolite by peroxidase, the glucuronidation in considered to be ..
  68. Patana A, Kurkela M, Finel M, Goldman A. Mutation analysis in UGT1A9 suggests a relationship between substrate and catalytic residues in UDP-glucuronosyltransferases. Protein Eng Des Sel. 2008;21:537-43 pubmed publisher
    ..The pair in human UGTs could be H37 and either D143 or D148 (UGT1A9 numbering). However, H37 is not totally conserved, being replaced by either Pro or Leu in UGT1A4 and UGT2B10...
  69. Kanai M, Tanabe S, Okada M, Suzuki H, Niki T, Katsuura M, et al. Polymorphisms of heme oxygenase-1 and bilirubin UDP-glucuronosyltransferase genes are not associated with Kawasaki disease susceptibility. Tohoku J Exp Med. 2003;200:155-9 pubmed
    ..There were no significant differences in the distribution of allele frequencies and genotypes of these polymorphisms between KD patients and controls. These polymorphisms are not associated with KD susceptibility. ..
  70. Chen G, Ramos E, Adeyemo A, Shriner D, Zhou J, Doumatey A, et al. UGT1A1 is a major locus influencing bilirubin levels in African Americans. Eur J Hum Genet. 2012;20:463-8 pubmed publisher
    ..In summary, UGT1A1 is a major locus influencing bilirubin levels and the results of this study promise to contribute to understanding of the etiology and treatment of hyperbilirubinaemia in African-ancestry populations. ..
  71. Kadakol A, Sappal B, Ghosh S, Lowenheim M, Chowdhury A, Chowdhury S, et al. Interaction of coding region mutations and the Gilbert-type promoter abnormality of the UGT1A1 gene causes moderate degrees of unconjugated hyperbilirubinaemia and may lead to neonatal kernicterus. J Med Genet. 2001;38:244-9 pubmed
  72. Mackenzie P, Owens I, Burchell B, Bock K, Bairoch A, Belanger A, et al. The UDP glycosyltransferase gene superfamily: recommended nomenclature update based on evolutionary divergence. Pharmacogenetics. 1997;7:255-69 pubmed
    ..g. UGT1A1*30) consistent with the Human Gene Nomenclature Guidelines. It is anticipated that this UGT gene nomenclature system will require updating on a regular basis. ..
  73. Gregory P, Gardner Stephen D, Lewinsky R, Duncliffe K, Mackenzie P. Cloning and characterization of the human UDP-glucuronosyltransferase 1A8, 1A9, and 1A10 gene promoters: differential regulation through an interior-like region. J Biol Chem. 2003;278:36107-14 pubmed
    ..UGT1A8 and 1A10 are expressed exclusively in the gastrointestinal tract, whereas UGT1A9 is expressed mainly in the liver and kidneys...
  74. Xiao L, Zhu L, Li W, Li C, Cao Y, Ge G, et al. New Insights into SN-38 Glucuronidation: Evidence for the Important Role of UDP Glucuronosyltransferase 1A9. Basic Clin Pharmacol Toxicol. 2017;: pubmed publisher
    ..and the selective inhibitor on SN-38 glucuronidation in pooled human liver microsomes (HLM) and recombinant UGT1A1/UGT1A9. For UGT1A1, SN-38 glucuronidation was little affected by BSA...
  75. Rowbotham S, Illingworth N, Daly A, Veal G, Boddy A. Role of UDP-glucuronosyltransferase isoforms in 13-cis retinoic acid metabolism in humans. Drug Metab Dispos. 2010;38:1211-7 pubmed publisher
    ..Further analysis revealed that UGT1A1, UGT1A3, UGT1A7, UGT1A8, and UGT1A9 were the major isoforms responsible for the glucuronidation of both substrates...
  76. Peer C, Sissung T, Kim A, Jain L, Woo S, Gardner E, et al. Sorafenib is an inhibitor of UGT1A1 but is metabolized by UGT1A9: implications of genetic variants on pharmacokinetics and hyperbilirubinemia. Clin Cancer Res. 2012;18:2099-107 pubmed publisher
    ..We hypothesized that sorafenib inhibits UGT1A1 and individuals carrying UGT1A1*28 and/or UGT1A9 variants experience greater sorafenib exposure and greater increase in sorafenib-induced plasma bilirubin ..
  77. Milton J, Sebastiani P, Solovieff N, Hartley S, Bhatnagar P, Arking D, et al. A genome-wide association study of total bilirubin and cholelithiasis risk in sickle cell anemia. PLoS ONE. 2012;7:e34741 pubmed publisher
    ..15 × 10(-4)). These results confirm that the UGT1A region is the major regulator of bilirubin metabolism in African Americans with sickle cell anemia, similar to what is observed in other ethnicities...
  78. Ritter J, Yeatman M, Kaiser C, Gridelli B, Owens I. A phenylalanine codon deletion at the UGT1 gene complex locus of a Crigler-Najjar type I patient generates a pH-sensitive bilirubin UDP-glucuronosyltransferase. J Biol Chem. 1993;268:23573-9 pubmed
    ..The low ion/pH requirements for bilirubin glucuronidation may signal the basis for the distribution of these isozymes to an organelle (endoplasmic reticulum) that can establish compatible conditions/compartments for each catalysis. ..
  79. Ramirez J, Mirkov S, Zhang W, Chen P, Das S, Liu W, et al. Hepatocyte nuclear factor-1 alpha is associated with UGT1A1, UGT1A9 and UGT2B7 mRNA expression in human liver. Pharmacogenomics J. 2008;8:152-61 pubmed
    ..investigates (1) whether the variability in HNF1alpha expression is associated with the variability in UGT1A1, UGT1A9 and UGT2B7 expression in human livers and (2) the functionality of 12 HNF1alpha variants using mRNA expression as ..
  80. Miura M, Kagaya H, Satoh S, Inoue K, Saito M, Habuchi T, et al. Influence of drug transporters and UGT polymorphisms on pharmacokinetics of phenolic glucuronide metabolite of mycophenolic acid in Japanese renal transplant recipients. Ther Drug Monit. 2008;30:559-64 pubmed publisher
    ..area under the plasma concentration-time curve (AUC) ratio of MPAG/MPA between UGT1A1, UGT1A6, UGT1A7, UGT1A8, and UGT1A9 I399C/T genotypes...
  81. Tougou K, Gotou H, Ohno Y, Nakamura A. Stereoselective glucuronidation and hydroxylation of etodolac by UGT1A9 and CYP2C9 in man. Xenobiotica. 2004;34:449-61 pubmed
    ..CYP2C9 therefore contributes to the stereoselective hydroxylation of R-etodolac. 3. Of several human UGT enzymes, UGT1A9 had the greatest activity for glucuronidation of S-etodolac...
  82. Martinez Balibrea E, Abad A, Martinez Cardus A, Gines A, Valladares M, Navarro M, et al. UGT1A and TYMS genetic variants predict toxicity and response of colorectal cancer patients treated with first-line irinotecan and fluorouracil combination therapy. Br J Cancer. 2010;103:581-9 pubmed publisher
    ..Genotyping of TYMS (5'TRP and 3'UTR), UGT1A1(*)28, UGT1A9(*)22 and UGT1A7(*)3 was performed in 149 metastatic CRC patients treated with irinotecan/5FU as first-line ..
  83. Ramirez J, Liu W, Mirkov S, Desai A, Chen P, Das S, et al. Lack of association between common polymorphisms in UGT1A9 and gene expression and activity. Drug Metab Dispos. 2007;35:2149-53 pubmed
    Interindividual variability in the glucuronidation of xenobiotics metabolized by UDP-glucuronosyltransferase 1A9 (UGT1A9) suggests the presence of functional UGT1A9 variants...
  84. Stachel N, Skopp G. Formation and inhibition of ethyl glucuronide and ethyl sulfate. Forensic Sci Int. 2016;265:61-4 pubmed publisher
    ..Resveratrol was a competitive inhibitor of UGT1A1, UGT1A9 and HLM; quercetin and kaempferol were inhibitors of all transferases under investigation except UGT2B15...
  85. Innocenti F, Liu W, Chen P, Desai A, Das S, Ratain M. Haplotypes of variants in the UDP-glucuronosyltransferase1A9 and 1A1 genes. Pharmacogenet Genomics. 2005;15:295-301 pubmed
    ..SN-38, the active metabolite of the anticancer agent irinotecan, is metabolized by both UGT1A1 and UGT1A9. We aim to characterize the UGT1A9-UGT1A1 haplotypes in Asians and Caucasians and gain insights on their ..
  86. Sanchez Fructuoso A, Maestro M, Calvo N, Viudarreta M, Perez Flores I, Veganzone S, et al. The prevalence of uridine diphosphate-glucuronosyltransferase 1A9 (UGT1A9) gene promoter region single-nucleotide polymorphisms T-275A and C-2152T and its influence on mycophenolic acid pharmacokinetics in stable renal transplant patients. Transplant Proc. 2009;41:2313-6 pubmed publisher
    The aim of this study was to evaluate the distribution of UGT1A9 promoter region T-275A and C-2152T single nucleotide polymorphisms (SNPs) in stable transplant patients and to investigate the impact of these SNPs on mycophenolic acid (MPA)..
  87. Korprasertthaworn P, Udomuksorn W, Yoovathaworn K. Three novel single nucleotide polymorphisms of UGT1A9 in a Thai population. Drug Metab Pharmacokinet. 2009;24:482-5 pubmed
    The human UDP-glucuronosyltransferase, UGT1A9, catalyzes glucuronidation of various endobiotics and xenobiotics...
  88. Thibaudeau J, Lepine J, Tojcic J, Duguay Y, Pelletier G, Plante M, et al. Characterization of common UGT1A8, UGT1A9, and UGT2B7 variants with different capacities to inactivate mutagenic 4-hydroxylated metabolites of estradiol and estrone. Cancer Res. 2006;66:125-33 pubmed
    ..In this study, we conducted functional analyses of genetic variants in the UDP-glucuronosyltransferase UGT1A8, UGT1A9, and UGT2B7 enzymes primarily involved in the inactivation of 4-OHCEs...
  89. Gao R, Li L, Xie C, Diao X, Zhong D, Chen X. Metabolism and pharmacokinetics of morinidazole in humans: identification of diastereoisomeric morpholine N+-glucuronides catalyzed by UDP glucuronosyltransferase 1A9. Drug Metab Dispos. 2012;40:556-67 pubmed publisher
    ..12 recombinant UDP glucuronosyltransferases (UGTs) indicated that this biotransformation was mainly catalyzed by UGT1A9. A kinetic study showed that N(+)-glucuronidation of racemic morinidazole in both HLMs and in UGT1A9 obeyed a ..
  90. den Braver Sewradj S, den Braver M, Baze A, Decorde J, Fonsi M, Bachellier P, et al. Direct comparison of UDP-glucuronosyltransferase and cytochrome P450 activities in human liver microsomes, plated and suspended primary human hepatocytes from five liver donors. Eur J Pharm Sci. 2017;109:96-110 pubmed publisher
    ..of a sensitive assay to phenotype activities of six major hepatic UGT isoforms (UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9 and UGT2B7) in intact PHH by analysis of glucuronidation of selective probe substrates...
  91. Harding D, Jeremiah S, Povey S, Burchell B. Chromosomal mapping of a human phenol UDP-glucuronosyltransferase, GNT1. Ann Hum Genet. 1990;54:17-21 pubmed
    ..The results indicate that this UDP-glucuronosyltransferase is encoded by a single gene, designated GNT1, located on human chromosome 2. ..
  92. Nishimura M, Ueda N, Naito S. Effects of dimethyl sulfoxide on the gene induction of cytochrome P450 isoforms, UGT-dependent glucuronosyl transferase isoforms, and ABCB1 in primary culture of human hepatocytes. Biol Pharm Bull. 2003;26:1052-6 pubmed
    ..CYP1B1, CYP2A6, CYP2E1, CYP3A4, CYP3A5, and CYP3A7), UGT-dependent glucuronosyl transferase isoforms (UGT1A6 and UGT1A9), and ABC transporter (ABCB1) after exposure to 0.1, 0.5, and 2.5% dimethyl sulfoxide (DMSO)...