Gene Symbol: UGT1A3
Description: UDP glucuronosyltransferase family 1 member A3
Alias: UDPGT, UDPGT 1-3, UGT-1C, UGT1-03, UGT1.3, UGT1A3S, UGT1C, UDP-glucuronosyltransferase 1-3, UDP glucuronosyltransferase 1 family, polypeptide A3, UDP glycosyltransferase 1 family, polypeptide A3, UDP-glucuronosyltransferase 1 family polypeptide A3s, UDP-glucuronosyltransferase 1-C, UDP-glucuronosyltransferase 1A3, UGT1*3
Species: human
Products:     UGT1A3

Top Publications

  1. Strassburg C, Manns M, Tukey R. Expression of the UDP-glucuronosyltransferase 1A locus in human colon. Identification and characterization of the novel extrahepatic UGT1A8. J Biol Chem. 1998;273:8719-26 pubmed exon 1-specific duplex reverse transcription-polymerase chain reaction revealed the expression of UGT1A1, UGT1A3, UGT1A4, UGT1A6, and UGT1A9 in the colon, which are also present in human liver...
  2. Strassburg C, Kneip S, Topp J, Obermayer Straub P, Barut A, Tukey R, et al. Polymorphic gene regulation and interindividual variation of UDP-glucuronosyltransferase activity in human small intestine. J Biol Chem. 2000;275:36164-71 pubmed
  3. 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. ..
  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. 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. ..
  6. 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. ..
  7. Böhmdorfer M, Szakmary A, Schiestl R, Vaquero J, Riha J, Brenner S, et al. Involvement of UDP-Glucuronosyltransferases and Sulfotransferases in the Excretion and Tissue Distribution of Resveratrol in Mice. Nutrients. 2017;9: pubmed publisher
    ..In summary, our data revealed organ-specific expression of Sults and Ugts in mice that strongly affects resveratrol concentrations; this may also be predictive in humans following oral uptake of dietary resveratrol. ..
  8. Zeng H, Li D, Qin X, Chen P, Tan H, Zeng X, et al. Hepatoprotective Effects of Schisandra sphenanthera Extract against Lithocholic Acid-Induced Cholestasis in Male Mice Are Associated with Activation of the Pregnane X Receptor Pathway and Promotion of Liver Regeneration. Drug Metab Dispos. 2016;44:337-42 pubmed publisher
    ..In conclusion, WZ has a protective effect against LCA-induced intrahepatic cholestasis, partially owing to activation of the PXR pathway and promotion of liver regeneration. ..
  9. Yamashita Y, Ueyama T, Nishi T, Yamamoto Y, Kawakoshi A, Sunami S, et al. Nrf2-inducing anti-oxidation stress response in the rat liver--new beneficial effect of lansoprazole. PLoS ONE. 2014;9:e97419 pubmed publisher
    ..e. the AhR/Cyp1a1/Nrf2 pathway in hepatocytes. ..

More Information

Publications132 found, 100 shown here

  1. Goetz F, Smith S, Goetz G, Murphy C. Sea lampreys elicit strong transcriptomic responses in the lake trout liver during parasitism. BMC Genomics. 2016;17:675 pubmed publisher
  2. Girard Bock C, Benoit Biancamano M, Villeneuve L, Desjardins S, Guillemette C. A Rare UGT2B7 Variant Creates a Novel N-Glycosylation Site at Codon 121 with Impaired Enzyme Activity. Drug Metab Dispos. 2016;44:1867-1871 pubmed
    ..Collectively, these variants have the potential to increase the proportion of variance explained in the UGT pathway resulting from changes in PTMs, such as N-linked glycosylation with consequences on drug metabolism. ..
  3. Li L, Huang X, Peng J, Zheng M, Zhong D, Zhang C, et al. Wedelolactone metabolism in rats through regioselective glucuronidation catalyzed by uridine diphosphate-glucuronosyltransferases 1As (UGT1As). Phytomedicine. 2016;23:340-9 pubmed publisher
    ..Multiple UGTs, including UGT1A1, UGT1A3, UGT1A6, UGT1A7, UGT1A8, UGT1A9, and UGT1A10, were involved in forming WEL glucuronides and O-methylated WEL ..
  4. Fang J, Han T, Wu Q, Beland F, Chang C, Guo L, et al. Differential gene expression in human hepatocyte cell lines exposed to the antiretroviral agent zidovudine. Arch Toxicol. 2014;88:609-23 pubmed publisher
  5. Wang C, Saar V, Leung K, Chen L, Wong G. Human amyloid ? peptide and tau co-expression impairs behavior and causes specific gene expression changes in Caenorhabditis elegans. Neurobiol Dis. 2018;109:88-101 pubmed publisher
    ..Taken together, our C. elegans double transgenic model provides insight on the fundamental neurobiologic processes underlying human AD and recapitulates selected transcriptomic changes observed in human AD brains. ..
  6. Liu J, Zhou Z, Zhang W, Bell M, Waalkes M. Changes in hepatic gene expression in response to hepatoprotective levels of zinc. Liver Int. 2009;29:1222-9 pubmed publisher
    ..Such gene expression changes, particularly the dramatic induction of MT and Nrf2 antioxidant pathway, occur in the absence of overt liver injury, and are probably important in the hepatoprotective effects of Zn against toxic insults. ..
  7. Hu D, Mackenzie P, Lu L, Meech R, McKinnon R. Induction of human UDP-Glucuronosyltransferase 2B7 gene expression by cytotoxic anticancer drugs in liver cancer HepG2 cells. Drug Metab Dispos. 2015;43:660-8 pubmed publisher
    ..g., epirubicin) and noncytotoxic drugs (e.g., morphine), which are UGT2B7 substrates. ..
  8. Hultman M, Song Y, Tollefsen K. 17α-Ethinylestradiol (EE2) effect on global gene expression in primary rainbow trout (Oncorhynchus mykiss) hepatocytes. Aquat Toxicol. 2015;169:90-104 pubmed publisher
    ..In conclusion, global transcriptional analysis demonstrated that EE2 affected a number of toxicologically relevant pathways associated with an estrogenic MoA in the rainbow trout hepatocytes. ..
  9. Coltell O, Asensio E, Sorli J, Barragán R, Fernández Carrión R, Portoles O, et al. Genome-Wide Association Study (GWAS) on Bilirubin Concentrations in Subjects with Metabolic Syndrome: Sex-Specific GWAS Analysis and Gene-Diet Interactions in a Mediterranean Population. Nutrients. 2019;11: pubmed publisher
    ..In conclusion, our study provides new data, with a gender perspective, on genes associated with total serum bilirubin concentrations in men and women, and suggests possible additional modulations by adherence to MedDiet. ..
  10. Ramprasath T, Selvam G. Potential impact of genetic variants in Nrf2 regulated antioxidant genes and risk prediction of diabetes and associated cardiac complications. Curr Med Chem. 2013;20:4680-93 pubmed
    ..Thus, the present review aims to explore the relationship between free radicals, diabetes and its associated complications with respect to the genetic makeup of Nrf2/ARE regulated genes in an effort to expand treatment options. ..
  11. Hankele A, Bauersachs S, Ulbrich S. Conjugated estrogens in the endometrium during the estrous cycle in pigs. Reprod Biol. 2018;18:336-343 pubmed publisher
  12. Saengtienchai A, Ikenaka Y, Kawata M, Kawai Y, Takeda K, Kondo T, et al. Comparison of xenobiotic metabolism in phase I oxidation and phase II conjugation between rats and bird species. Comp Biochem Physiol C Toxicol Pharmacol. 2018;214:28-35 pubmed publisher
    ..Characterization of xenobiotic metabolism revealed species differences between birds and mammals, raising concerns about exposure to various xenobiotics in the environment. ..
  13. Tsai M, Wang Y, Lai Y, Tsou H, Liou G, Ko J, et al. Kaempferol protects against propacetamol-induced acute liver injury through CYP2E1 inactivation, UGT1A1 activation, and attenuation of oxidative stress, inflammation and apoptosis in mice. Toxicol Lett. 2018;290:97-109 pubmed publisher
    ..These data suggested that kaempferol protects the liver against propacetamol-induced injury through anti-oxidative, anti-inflammatory and anti-apoptotic activities. ..
  14. Korprasertthaworn P, Polasek T, Sorich M, McLachlan A, Miners J, Tucker G, et al. In Vitro Characterization of the Human Liver Microsomal Kinetics and Reaction Phenotyping of Olanzapine Metabolism. Drug Metab Dispos. 2015;43:1806-14 pubmed publisher
    ..In addition to CYP1A2-mediated OLZ-N-demethylation, these results suggest that other P450 enzymes, particularly CYP2C8, contribute significantly to oxidative OLZ metabolism through catalysis of OLZ-N-demethylation. ..
  15. Zhang C, Pang Y, Zhang Q, Huang G, Xu M, Tang B, et al. Hemolymph transcriptome analysis of Chinese mitten crab (Eriocheir sinensis) with intact, left cheliped autotomy and bilateral eyestalk ablation. Fish Shellfish Immunol. 2018;81:266-275 pubmed publisher
    ..Our research obtained abundant E. sinensis hemolymph transcriptome information by RNA-Seq, which provides multi-level information for the cloning of novel genes and the study of hemolymph molecular immunology mechanisms of E. sinensis. ..
  16. Iwamura A, Watanabe K, Akai S, Nishinosono T, Tsuneyama K, Oda S, et al. Zomepirac Acyl Glucuronide Is Responsible for Zomepirac-Induced Acute Kidney Injury in Mice. Drug Metab Dispos. 2016;44:888-96 pubmed publisher
    ..This is the first study to demonstrate that AG accumulation in the kidney by TOTP and BSO treatment could explain renal toxicity and to show the in vivo toxicological potential of AGs. ..
  17. Ho M, Ring N, Amaral K, Doshi U, Li A. Human Enterocytes as an In Vitro Model for the Evaluation of Intestinal Drug Metabolism: Characterization of Drug-Metabolizing Enzyme Activities of Cryopreserved Human Enterocytes from Twenty-Four Donors. Drug Metab Dispos. 2017;45:686-691 pubmed publisher
  18. Greer A, Dates C, Starlard Davenport A, Edavana V, Bratton S, Dhakal I, et al. A potential role for human UDP-glucuronosyltransferase 1A4 promoter single nucleotide polymorphisms in the pharmacogenomics of tamoxifen and its derivatives. Drug Metab Dispos. 2014;42:1392-400 pubmed publisher
    ..These alterations in glucuronidation may lead to prolonged circulating half-lives and may potentially modify the effectiveness of these drugs in the treatment of breast cancer. ..
  19. Li Q, Wang L, Dai P, Zeng X, Qi X, Zhu L, et al. A combined strategy of mass fragmentation, post-column cobalt complexation and shift in ultraviolet absorption spectra to determine the uridine 5'-diphospho-glucuronosyltransferase metabolism profiling of flavones after oral administration of a flavo. J Chromatogr A. 2015;1395:116-28 pubmed publisher
    ..4h, except for the concentration of luteolin 3'-glucronide (approximately 9h). Rat exposure was practically non-linear under the studied dosages (200 to 400mg/kg). ..
  20. Hong B, Su Z, Zhang C, Yang Y, Guo Y, Li W, et al. Reserpine Inhibit the JB6 P+ Cell Transformation Through Epigenetic Reactivation of Nrf2-Mediated Anti-oxidative Stress Pathway. AAPS J. 2016;18:659-69 pubmed publisher
  21. 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
    ..The major metabolites were two diastereoisomeric N(+)-glucuronides, and UGT1A9 played an important role in N(+)-glucuronidation. ..
  22. Dong S, Ji J, Hu L, Wang H. Dihydromyricetin alleviates acetaminophen-induced liver injury via the regulation of transformation, lipid homeostasis, cell death and regeneration. Life Sci. 2019;: pubmed publisher
    ..Based on these findings, DHM provides a potential and novel approach for preventing and treating APAP-induced liver damage, and SREBP-1c signalling might be a new therapeutic target for APAP hepatotoxicity. ..
  23. Szultka Mlynska M, Buszewski B. Study of in-vitro metabolism of selected antibiotic drugs in human liver microsomes by liquid chromatography coupled with tandem mass spectrometry. Anal Bioanal Chem. 2016;408:8273-8287 pubmed
    ..Finally, LC-MS/MS spectrometry was revealed to be a suitable analytical tool to procure a feasible analytical base for the envisioned in vivo experiments. Graphical Abstract Workflow overview of in vitro drug metabolism studies. ..
  24. Chen S, Tukey R. Humanized UGT1 Mice, Regulation of UGT1A1, and the Role of the Intestinal Tract in Neonatal Hyperbilirubinemia and Breast Milk-Induced Jaundice. Drug Metab Dispos. 2018;46:1745-1755 pubmed publisher
    ..Our findings outline a new model that includes an active intestinal ROS /IκB kinase/nuclear receptor corepressor 1 loop that can be applied to an understanding of breast milk-induced jaundice. ..
  25. Magdalou J, Totis M, Boiteux Antoine A, Fournel Gigleux S, Siest G, Schladt L, et al. Effect of 1-benzylimidazole on cytochromes P-450 induction and on the activities of epoxide hydrolases and UDP-glucuronosyltransferases in rat liver. Biochem Pharmacol. 1988;37:3297-304 pubmed
    ..These observations emphasize the variety of the effects of 1-benzylimidazole on drug-metabolizing enzymes. ..
  26. Talavera Pons S, Boyer A, Lamblin G, Chennell P, Châtenet F, Nicolas C, et al. Managing drug-drug interactions with new direct-acting antiviral agents in chronic hepatitis C. Br J Clin Pharmacol. 2017;83:269-293 pubmed publisher
    ..The key to interpret DDI data is a good understanding of the pharmacokinetic profiles of the drugs involved. Their ability to inhibit CYP450-3A4 and transporters (hepatic and/or intestinal) can have significant clinical consequences...
  27. Kabeya T, Qiu S, Hibino M, Nagasaki M, Kodama N, Iwao T, et al. Cyclic AMP Signaling Promotes the Differentiation of Human Induced Pluripotent Stem Cells into Intestinal Epithelial Cells. Drug Metab Dispos. 2018;46:1411-1419 pubmed publisher
    ..This study is the first to report that the activation of cAMP signaling promotes differentiation of human iPS cell-derived intestinal epithelial cells. ..
  28. Huang C, Chen H, Lin T, Lin A, Lii C. Shikonin upregulates the expression of drug-metabolizing enzymes and drug transporters in primary rat hepatocytes. J Ethnopharmacol. 2018;216:18-25 pubmed publisher
    ..Moreover, Nrf2 activation is dependent on mitogen-activated protein kinases. ..
  29. Cai S, Hou N, Zhao G, Liu X, He Y, Liu H, et al. Nrf2 Is a Key Regulator on Puerarin Preventing Cardiac Fibrosis and Upregulating Metabolic Enzymes UGT1A1 in Rats. Front Pharmacol. 2018;9:540 pubmed publisher
    ..Autoregulatory circuits between puerarin and Nrf2-regulated UGT1A1 attenuates side effects associated with treatment, but it does not weaken puerarin's pharmacological effects. ..
  30. Oeser S, Bingham J, Collier A. Regulation of Hepatic UGT2B15 by Methylation in Adults of Asian Descent. Pharmaceutics. 2018;10: pubmed publisher
    ..The UGT1A3 mRNA was 2-fold higher in females than males (p < 0...
  31. Hanioka N, Ohkawara S, Isobe T, Ochi S, Tanaka Kagawa T, Jinno H. Regioselective glucuronidation of daidzein in liver and intestinal microsomes of humans, monkeys, rats, and mice. Arch Toxicol. 2018;92:2809-2817 pubmed publisher
  32. Chen C, Han Y, Yang Z, Rodrigues A. Effect of interferon-?2b on the expression of various drug-metabolizing enzymes and transporters in co-cultures of freshly prepared human primary hepatocytes. Xenobiotica. 2011;41:476-85 pubmed publisher
  33. Sane R, Steinmann G, Huang Q, Li Y, Podila L, Mease K, et al. Mechanisms underlying benign and reversible unconjugated hyperbilirubinemia observed with faldaprevir administration in hepatitis C virus patients. J Pharmacol Exp Ther. 2014;351:403-12 pubmed publisher
    ..As such, faldaprevir-mediated hyperbilirubinemia is not associated with any liver injury or toxicity, and is considered to result from decreased bilirubin elimination due to a drug-bilirubin interaction. ..
  34. 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
    ..3-fold at 30 ?mol/L) and weakly induced ABCB11, CYP2C19 and UGT1A3. In contrast, telaprevir had no significant influence on mRNA expression of CYP3A4, UGT1A9, ABCB1, ABCC2 and ..
  35. Nomura A, Maruo Y, Taga T, Takeuchi Y. Contribution of UGT1A1 variations to chemotherapy-induced unconjugated hyperbilirubinemia in pediatric leukemia patients. Pediatr Res. 2016;80:252-7 pubmed publisher
    ..Therefore, it is not necessary to cease chemotherapy in patients with these mutations who develop unconjugated hyperbilirubinemia without associated liver dysfunction. ..
  36. He G, Troberg J, Lv X, Xia Y, Zhu L, Ning J, et al. Identification and characterization of human UDP-glucuronosyltransferases responsible for xanthotoxol glucuronidation. Xenobiotica. 2018;48:109-116 pubmed publisher
    ..The other enzymes, namely UGT1A3, UGT1A1, UGT1A6, UGT1A10 (commercial), and UGT2B7 displayed moderate-to-low reaction rates. 4...
  37. Achour B, Dantonio A, Niosi M, Novak J, Al Majdoub Z, Goosen T, et al. Data Generated by Quantitative Liquid Chromatography-Mass Spectrometry Proteomics Are Only the Start and Not the Endpoint: Optimization of Quantitative Concatemer-Based Measurement of Hepatic Uridine-5'-Diphosphate-Glucuronosyltransferase Enzymes wit. Drug Metab Dispos. 2018;46:805-812 pubmed publisher
    ..34). No spurious abundance-activity relationships were identified. However, methods remained suboptimal for UGT1A3 and UGT1A9; here hydrophobicity of standard peptides is believed to be limiting...
  38. Shi X, Zhang G, Mackie B, Yang S, Wang J, Shan L. Comparison of the in vitro metabolism of psoralidin among different species and characterization of its inhibitory effect against UDP- glucuronosyltransferase (UGT) or cytochrome p450 (CYP450) enzymes. J Chromatogr B Analyt Technol Biomed Life Sci. 2016;1029-1030:145-156 pubmed publisher
    ..CYP2C19 played a key role in the metabolism of psorslidin in human liver microsomes. These findings could be used to advance the understanding of psoralidin. ..
  39. Papageorgiou I, Freytsis M, Court M. Transcriptome association analysis identifies miR-375 as a major determinant of variable acetaminophen glucuronidation by human liver. Biochem Pharmacol. 2016;117:78-87 pubmed publisher
    ..Thus miR-375 is identified as a novel repressor of UGT1A-mediated hepatic acetaminophen glucuronidation through reduced AhR expression, which could predispose some individuals to increased risk for acetaminophen-induced ALF. ..
  40. Iwamura A, Nakajima M, Oda S, Yokoi T. Toxicological potential of acyl glucuronides and its assessment. Drug Metab Pharmacokinet. 2017;32:2-11 pubmed publisher
    ..In addition to in vitro studies, studies in model animals indicate the in vivo toxicological potential of AGs and help understand the mechanisms of the AG toxicity. ..
  41. Yabusaki R, Iwano H, Tsushima S, Koike N, Ohtani N, Tanemura K, et al. Weak activity of UDP-glucuronosyltransferase toward Bisphenol analogs in mouse perinatal development. J Vet Med Sci. 2015;77:1479-84 pubmed publisher
    ..In conclusion, BPAF possibly tends to accumulate in the fetus, because of weak metabolism during the perinatal period, suggesting that the metabolism of individual Bisphenol analogs requires assessment to properly gauge their risks. ..
  42. Gao R, Liu M, Chen Y, Xia C, Zhang H, Xiong Y, et al. Identification and characterization of human UDP-glucuronosyltransferases responsible for the in vitro glucuronidation of ursolic acid. Drug Metab Pharmacokinet. 2016;31:261-8 pubmed publisher
    ..33 ± 0.03 and 0.42 ± 0.03 nmol/min/(mg protein). Among the 12 recombinant UGT enzymes investigated, UGT1A3 and UGT1A4 were identified as the major enzymes catalyzing the glucuronidation of UA [Km values of 2.58 ± 0...
  43. Mei S, Feng W, Zhu L, Yu Y, Yang W, Gao B, et al. Genetic polymorphisms and valproic acid plasma concentration in children with epilepsy on valproic acid monotherapy. Seizure. 2017;51:22-26 pubmed publisher
    ..rs28898617 (UGT1A3/4/5/6/7/8/9/10, BETA=0.32, P=0.0089) was significantly associated with higher lnCDRV...
  44. Yang N, Li S, Yan C, Sun R, He J, Xie Y, et al. Inhibitory Effects of Endogenous Linoleic Acid and Glutaric Acid on the Renal Glucuronidation of Berberrubine in Mice and on Recombinant Human UGT1A7, 1A8, and 1A9. Mol Pharmacol. 2018;93:216-227 pubmed publisher
    ..It has been suggested that the endogenous molecules have the potential to affect the efficiency of glucuronidation, which might be a key factor contributing to individual differences in drug metabolism. ..
  45. Liu X, Sheng L, Zhao M, Mi J, Liu Z, Li Y. In vitro glucuronidation of the primary metabolite of 10-chloromethyl-11-demethyl-12-oxo-calanolide A by human liver microsomes and its interactions with UDP-glucuronosyltransferase substrates. Drug Metab Pharmacokinet. 2015;30:89-96 pubmed publisher
    ..8 μM. The results suggest that UGT1A1 provides the major contribution to M3 glucuronidation in vitro and M3 has the potential to interact with xenobiotics and endogenous chemicals that are UGT1A9 and UGT 2B7 substrates. ..
  46. Ikuta H, Kawase A, Iwaki M. Stereoselective Pharmacokinetics and Chiral Inversion of Ibuprofen in Adjuvant-induced Arthritic Rats. Drug Metab Dispos. 2017;45:316-324 pubmed publisher
    ..These results suggested that AA could affect drug efficacies after stereoselective changes in the pharmacokinetics of R-IB and S-IB. ..
  47. Oates C, Koenig D, Rhyne J, Bogush N, O CONNELL J, Mitchell B, et al. Novel polymorphisms associated with hyperalphalipoproteinemia and apparent cardioprotection. J Clin Lipidol. 2018;12:110-115 pubmed publisher
    ..Depletion to estimate the predictive effect of each nsSNP on the gene product, rare, deleterious polymorphisms in UGT1A3, PLLP, PLEKHH1, ANK2, DIS3L, ACACB, and LRP4 were identified in 16 subjects with HALP but not in any tested ..
  48. Barbier O, Albert C, Martineau I, Vallee M, High K, Labrie F, et al. Glucuronidation of the nonsteroidal antiestrogen EM-652 (SCH 57068), by human and monkey steroid conjugating UDP-glucuronosyltransferase enzymes. Mol Pharmacol. 2001;59:636-45 pubmed date, the two EM-652-monoglucuronides were detected after incubation with microsomes containing human UGT1A1, UGT1A3, UGT1A8, UGT1A9, and monkey monUGT1A01, monUGT1A03, and monUGT1A09...
  49. Cheng Y, Zhou J, Wang M, Liu Y, Guo B, Chen B. Single-shot multi-reaction monitoring of intact marker conjugates for quantitative profiling of human major microsomal glucuronidations and its utility to screen inhibitors from medicinal herbs. Anal Bioanal Chem. 2016;408:8117-8132 pubmed
    ..Graphical abstract Multi-reaction monitoring of intact conjugate metabolites for quantitative profiling of human major glucuronidations. ..
  50. 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
    ..IC50 values for the inhibition of all UGT1A enzymes, except UGT1A3 and UGT1A4, by the four KIs were <10?M...
  51. Hanioka N, Isobe T, Kinashi Y, Tanaka Kagawa T, Jinno H. Hepatic and intestinal glucuronidation of mono(2-ethylhexyl) phthalate, an active metabolite of di(2-ethylhexyl) phthalate, in humans, dogs, rats, and mice: an in vitro analysis using microsomal fractions. Arch Toxicol. 2016;90:1651-7 pubmed publisher
  52. Dluzen D, Sutliff A, Chen G, Watson C, Ishmael F, Lazarus P. Regulation of UGT2B Expression and Activity by miR-216b-5p in Liver Cancer Cell Lines. J Pharmacol Exp Ther. 2016;359:182-93 pubmed publisher
    ..This is the first evidence that miRNAs regulate UGT 2B7, 2B4, and 2B10 expression, and that miR-216b-5p regulation of UGT2B proteins may be important in regulating the metabolism of UGT2B substrates. ..
  53. Gu B, Laborda P, Wei S, Duan X, Song H, Liu L, et al. Discovery and Biochemical Characterization of the UDP-Xylose Biosynthesis Pathway in Sphaerobacter thermophilus. Protein Pept Lett. 2016;23:1103-1110 pubmed
    ..The biosynthetic potential of StUGD was further exemplified in a coupled enzymatic reaction with an UDP-glucuronosyltransferase, allowing the glucuronylation of the natural model substrate bilirubin. ..
  54. Ishimaru S, Yuza Y, Kaneko T, Urashima M. Effect of UGT2B17 deletion polymorphism on prognosis in pediatric cancer. Pediatr Int. 2017;59:427-431 pubmed publisher
    ..0004). UGT2B17 deletion polymorphism may improve the relapse-free rate in children with non-lymphoblastic malignancy. ..
  55. Owen M, McCarty K, Hart C, Steadman C, Lemley C. Endometrial blood perfusion as assessed using a novel laser Doppler technique in Angus cows. Anim Reprod Sci. 2018;190:119-126 pubmed publisher
  56. Chen L, Yu M, Wu Q, Peng Z, Wang D, Kuca K, et al. Gender and geographical variability in the exposure pattern and metabolism of deoxynivalenol in humans: a review. J Appl Toxicol. 2017;37:60-70 pubmed publisher
    ..In this review, we provide global information on DON metabolism, human exposure and gender differences in humans. Also, control strategies for this mycotoxin are discussed. Copyright © 2016 John Wiley & Sons, Ltd...
  57. Ran R, Zhang C, Li R, Chen B, Zhang W, Zhao Z, et al. Evaluation and Comparison of the Inhibition Effect of Astragaloside IV and Aglycone Cycloastragenol on Various UDP-Glucuronosyltransferase (UGT) Isoforms. Molecules. 2016;21: pubmed
    ..034 μM and 20.98 μM, respectively. ..
  58. 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
    ..Our work provides unprecedented evidence for a functional interaction between glucuronidation and bioenergetic metabolism. ..
  59. Matic M, de Wildt S, Tibboel D, van Schaik R. Analgesia and Opioids: A Pharmacogenetics Shortlist for Implementation in Clinical Practice. Clin Chem. 2017;63:1204-1213 pubmed publisher
    ..The application of PGx in the management of pain with opioids has the potential to improve therapy. We provide a shortlist of 10 genes that are the most promising markers for clinical use in this context. ..
  60. Isobe T, Ohkawara S, Ochi S, Tanaka Kagawa T, Jinno H, Hanioka N. Naringenin glucuronidation in liver and intestine microsomes of humans, monkeys, rats, and mice. Food Chem Toxicol. 2018;111:417-422 pubmed publisher
    ..These results suggest that the metabolic abilities and regioselectivity of UGT enzymes toward naringenin in the liver and intestines generally differ between primates and rodents. ..
  61. Chen Y, Chen S, Li X, Wang X, Zeng S. Genetic variants of human UGT1A3: functional characterization and frequency distribution in a Chinese Han population. Drug Metab Dispos. 2006;34:1462-7 pubmed
    ..quercetin, luteolin, and kaempferol, were used as substrates for glucuronidation by wild-type and variant UGT1A3s. Our results demonstrated that the activities of three variants, UGT1A3.2, UGT1A3.3, and UGT1A3...
  62. Goey A, Figg W. UGT genotyping in belinostat dosing. Pharmacol Res. 2016;105:22-7 pubmed publisher
    ..Clinical effects of this genotype-based dosing recommendation is currently prospectively being investigated. Overall, the data suggest that UGT1A1 genotyping is useful for improving belinostat therapy. ..
  63. Papageorgiou I, Court M. Identification and validation of microRNAs directly regulating the UDP-glucuronosyltransferase 1A subfamily enzymes by a functional genomics approach. Biochem Pharmacol. 2017;137:93-106 pubmed publisher
    ..Finally, miR-21-3p and miR-200a-3p expression were negatively correlated with UGT1A6 activity and mRNA in human liver samples. Thus, UGT1A is regulated by multiple miRNAs with some showing allele-dependent effects. ..
  64. Kahma H, Filppula A, Neuvonen M, Tarkiainen E, Tornio A, Holmberg M, et al. Clopidogrel Carboxylic Acid Glucuronidation is Mediated Mainly by UGT2B7, UGT2B4, and UGT2B17: Implications for Pharmacogenetics and Drug-Drug Interactions . Drug Metab Dispos. 2018;46:141-150 pubmed publisher
    ..42 and 2.82 µl⋅min-1⋅mg-1, respectively. Of other enzymes displaying activity (UGT1A3, UGT1A9, UGT1A10-H, and UGT2B4), UGT2B4 (CLint,u 0...
  65. Chen X, Li R, Geng Z. Cold stress initiates the Nrf2/UGT1A1/L-FABP signaling pathway in chickens. Poult Sci. 2015;94:2597-603 pubmed publisher
  66. Mojarrabi B, Butler R, Mackenzie P. cDNA cloning and characterization of the human UDP glucuronosyltransferase, UGT1A3. Biochem Biophys Res Commun. 1996;225:785-90 pubmed
    The cDNA encoding the UDP glucuronosyltransferase, UGT1A3, has been cloned and expressed in cell culture...
  67. 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 ..
  68. Hou C, Liu W, Liang Z, Han W, Li J, Ye L, et al. UGT-mediated metabolism plays a dominant role in the pharmacokinetic behavior and the disposition of morusin in vivo and in vitro. J Pharm Biomed Anal. 2018;154:339-353 pubmed publisher
    ..Clearance rates of M-4'-G in HLM, RLM, UGT1A1, UGT1A3, and UGT2B7 were 137.02, 127.55, 32.54, 41.18, and 35.07?ml/min/mg, respectively...
  69. Yilmaz L, Borazan E, Aytekin T, Baskonus I, Aytekin A, Oztuzcu S, et al. Increased UGT1A3 and UGT1A7 expression is associated with pancreatic cancer. Asian Pac J Cancer Prev. 2015;16:1651-5 pubmed
    ..UGT1A isoforms are expressed tissue specifically. The aim of this study was to examine the relationship between UGT1A3 and UGT1A7 mRNA expression and pancreatic cancer...
  70. You B, Gong E, Choi Y. Inhibitory Effect of Sauchinone on UDP-Glucuronosyltransferase (UGT) 2B7 Activity. Molecules. 2018;23: pubmed publisher
    ..Our results indicated that there is potential HDI between sauchinone and drugs undergoing UGT2B7-mediated metabolism, possibly contributing to the safe use of sauchinone and drug combinations. ..
  71. Strassburg C, Oldhafer K, Manns M, Tukey R. Differential expression of the UGT1A locus in human liver, biliary, and gastric tissue: identification of UGT1A7 and UGT1A10 transcripts in extrahepatic tissue. Mol Pharmacol. 1997;52:212-20 pubmed
    ..b>UGT1A3 and UGT1A6 were found to be expressed in the three tissues, whereas UGT1A5 and UGT1A8 were not expressed...
  72. Gong Q, Cho J, Huang T, Potter C, Gholami N, Basu N, et al. Thirteen UDPglucuronosyltransferase genes are encoded at the human UGT1 gene complex locus. Pharmacogenetics. 2001;11:357-68 pubmed
    ..The mRNAs are differentially expressed in hepatic and extrahepatic tissues. This locus is indeed novel, indicating the least usage of exon sequences in specifying different transferase isozymes that have an expansive substrate range. ..
  73. Hong M, Karlsson R, Magnusson P, Lewis M, Isaacs W, Zheng L, et al. A genome-wide assessment of variability in human serum metabolism. Hum Mutat. 2013;34:515-24 pubmed publisher
    ..mQTL SNPs and mQTL-harboring genes were over-represented across GWASs conducted to date, suggesting that these data may have utility in tracing the molecular basis of some complex disease associations. ..
  74. Migita T, Takayama K, Urano T, Obinata D, Ikeda K, Soga T, et al. ACSL3 promotes intratumoral steroidogenesis in prostate cancer cells. Cancer Sci. 2017;108:2011-2021 pubmed publisher
    ..These findings suggest that ACSL3 contributes to the growth of CRPC through intratumoral steroidogenesis (i.e. promoting androgen synthesis from DHEAS and preventing the catabolism of active androgens). ..
  75. Weiss J, Kocher J, Mueller C, Rosenzweig S, Theile D. Impact of enzalutamide and its main metabolite N-desmethyl enzalutamide on pharmacokinetically important drug metabolizing enzymes and drug transporters. Biopharm Drug Dispos. 2017;38:517-525 pubmed publisher
    ..chain reaction, our study demonstrated a concentration-dependent induction of CYP1A1, CYP1A2, CYP3A5, CYP3A4, UGT1A3, UGT1A9, ABCB1, ABCC2 and ABCG2 mRNA...
  76. Cheng X, Lv X, Qu H, Li D, Hu M, Guo W, et al. Comparison of the inhibition potentials of icotinib and erlotinib against human UDP-glucuronosyltransferase 1A1. Acta Pharm Sin B. 2017;7:657-664 pubmed publisher
  77. Kuehl G, Murphy S. N-glucuronidation of nicotine and cotinine by human liver microsomes and heterologously expressed UDP-glucuronosyltransferases. Drug Metab Dispos. 2003;31:1361-8 pubmed
    ..97 (p < 0.0001). The glucuronidation of nicotine and cotinine by heterologously expressed UGT1A3, UGT1A4, and UGT1A9 was also determined. All three enzymes catalyzed the glucuronidation of nicotine...
  78. 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)...
  79. 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
    ..Furthermore, in the presence of BSA, magnolol, a selective UGT1A9 inhibitor, displays moderate inhibition against HLM. Results together conclude that UGT1A9 serves as an additional important contributor to hepatic SN-38 glucuronidation...
  80. Konishi K, Tenmizu D, Takusagawa S. Identification of Uridine 5'-Diphosphate-Glucuronosyltransferases Responsible for the Glucuronidation of Mirabegron, a Potent and Selective ?3-Adrenoceptor Agonist, in Human Liver Microsomes. Eur J Drug Metab Pharmacokinet. 2018;43:301-309 pubmed publisher
    ..UGT2B7 is the main catalyst of M11 formation in HLMs. Regarding M13 and M14 formation, UGT1A3 and UGT1A8 are strong candidates for glucuronidation, respectively.
  81. Moghrabi N, Sutherland L, Wooster R, Povey S, Boxer M, Burchell B. Chromosomal assignment of human phenol and bilirubin UDP-glucuronosyltransferase genes (UGT1A-subfamily). Ann Hum Genet. 1992;56:81-91 pubmed
    ..The results obtained indicate that all four cDNA clones are encoded by gene(s) located on human chromosome 2. ..
  82. 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. ..
  83. 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...
  84. 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
    ..SNPs in UGT1A1, UGT1A3, UGT1A6, UGT1A8 and UGT1A10, different isoforms within the UGT1A locus, were identified (most significant rs887829,..
  85. Wang Y, Li Q, Dai Y, Pan R, Xia Y. Development of a LC-MS/MS method to investigate the interference of pharmacokinetics of the main constituents in Saxifraga stolonifera: Involvement of drug metabolism enzymes. J Pharm Biomed Anal. 2018;148:128-135 pubmed publisher
    ..extract, significantly decreased the glucuronidation of bergenin through inhibiting the activities of UGT1A1 and UGT1A3, and reduced the metabolism of protocatechuic acid by inhibiting the activity of catechol-O-methyltransferase...
  86. Asai Y, Sakakibara Y, Nadai M, Katoh M. Effect of carbamazepine on expression of UDP-glucuronosyltransferase 1A6 and 1A7 in rat brain. Drug Metab Pharmacokinet. 2017;32:286-292 pubmed publisher
    ..Histone H3 lysine 9 acetylation, H3 lysine 4 pan-methylation, and H3 lysine 9 mono-methylation may not be required for the induction. This study clarified that CBZ affected Ugt1a6 and Ugt1a7 in the brain. ..
  87. Tong Z, Yerramilli U, Surapaneni S, Kumar G. The interactions of lenalidomide with human uptake and efflux transporters and UDP-glucuronosyltransferase 1A1: lack of potential for drug-drug interactions. Cancer Chemother Pharmacol. 2014;73:869-74 pubmed publisher
    ..In addition, inhibition of UDP-glucuronosyltransferase 1A1 (UGT1A1) variants by lenalidomide was also assessed...
  88. Guan H, Li P, Wang X, Yue J, He Y, Luo X, et al. Shengjiang Xiexin Decoction Alters Pharmacokinetics of Irinotecan by Regulating Metabolic Enzymes and Transporters: A Multi-Target Therapy for Alleviating the Gastrointestinal Toxicity. Front Pharmacol. 2017;8:769 pubmed publisher
    ..And the underlying mechanism of drug interaction between CPT-11 and SXD involves decreasing hepatic Mrp-2 and P-gp expression and altering the activities of CES and UGT...
  89. Green M, King C, Mojarrabi B, Mackenzie P, Tephly T. Glucuronidation of amines and other xenobiotics catalyzed by expressed human UDP-glucuronosyltransferase 1A3. Drug Metab Dispos. 1998;26:507-12 pubmed
    ..b>UGT1A3 is 93% identical to UGT1A4 in primary amino acid sequence...
  90. Lampen A, Ebert B, Stumkat L, Jacob J, Seidel A. Induction of gene expression of xenobiotic metabolism enzymes and ABC-transport proteins by PAH and a reconstituted PAH mixture in human Caco-2 cells. Biochim Biophys Acta. 2004;1681:38-46 pubmed
    ..We conclude that B[a]P, chrysene, B[k]F, and DB[a,l]P have specific effects on intestinal CYP1A1, CYP1B1, UGT1A6, and UDP1A7 mRNA expression but no effects on the expression of SULT...
  91. Zhou Z, Lu Y, Song G, Wang Y, Chen J, Xiao C, et al. In Vitro Study on Influences of UGT1A8 Gene Polymorphisms on Mycophenolate Mofetil Metabolism. Exp Clin Transplant. 2018;16:466-472 pubmed publisher
    ..0569). Our results showed that UGT1A8 gene polymorphisms can affect the activity of UDP glucuronosyltransferase enzyme, which may influence the elimination of mycophenolate mofetil in different patients. ..
  92. Fujiwara R, Yoda E, Tukey R. Species differences in drug glucuronidation: Humanized UDP-glucuronosyltransferase 1 mice and their application for predicting drug glucuronidation and drug-induced toxicity in humans. Drug Metab Pharmacokinet. 2018;33:9-16 pubmed publisher
    ..In this review article, studies of drug metabolism and toxicity in the hUGT1 mice are summarized. We further discuss research and strategic directions to advance the understanding of drug glucuronidation in humans. ..