UGT2B4

Summary

Gene Symbol: UGT2B4
Description: UDP glucuronosyltransferase family 2 member B4
Alias: HLUG25, UDPGT2B4, UDPGTH1, UDPGTh-1, UGT2B11, UDP-glucuronosyltransferase 2B4, UDP glucuronosyltransferase 2 family, polypeptide B4, UDP-glucuronyltransferase, family 2, beta-4, UDPGT 2B4, hyodeoxycholic acid, hyodeoxycholic acid-specific UDPGT
Species: human
Products:     UGT2B4

Top Publications

  1. Levesque E, Beaulieu M, Hum D, Belanger A. Characterization and substrate specificity of UGT2B4 (E458): a UDP-glucuronosyltransferase encoded by a polymorphic gene. Pharmacogenetics. 1999;9:207-16 pubmed
    ..UGT2B4(E458) conjugates hyodeoxycholic acid (HDCA) as well as 4-hydroxyestrone (4-OH-E1), androstane-3alpha,17beta-diol (3alpha-diol) and androsterone (..
  2. Yang F, Wang Y, Li G, Xue J, Chen Z, Jin F, et al. Effects of corilagin on alleviating cholestasis via farnesoid X receptor-associated pathways in vitro and in vivo. Br J Pharmacol. 2018;175:810-829 pubmed publisher
    ..Real-time PCR and Western blotting were employed to detect the mRNA and protein levels of FXR, SHP1, SHP2, UGT2B4, BSEP, CYP7A1, CYP7B1, NTCP, MRP2 and SULT2A1...
  3. Liu W, Ramirez J, Gamazon E, Mirkov S, Chen P, Wu K, et al. Genetic factors affecting gene transcription and catalytic activity of UDP-glucuronosyltransferases in human liver. Hum Mol Genet. 2014;23:5558-69 pubmed publisher
    ..Transcription levels of five major hepatic UGT1A (UGT1A1, UGT1A3, UGT1A4, UGT1A6 and UGT1A9) and five UGT2B (UGT2B4, UGT2B7, UGT2B10, UGT2B15 and UGT2B17) genes were quantified in human liver tissue samples (n = 125) using real-..
  4. Badée J, Qiu N, Parrott N, Collier A, Schmidt S, Fowler S. Optimization of Experimental Conditions of Automated Glucuronidation Assays in Human Liver Microsomes Using a Cocktail Approach and Ultra-High Performance Liquid Chromatography-Tandem Mass Spectrometry. Drug Metab Dispos. 2019;47:124-134 pubmed publisher
    ..Hepatic glucuronidation activities of UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, UGT2B4, UGT2B7, UGT2B10, UGT2B15, and UGT2B17 were determined using cocktail incubations of 10 UGT probe substrates...
  5. 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. CT was extensively metabolized by UGTs following metabolism by CYPs in the liver.
  6. Chen X, Wang Y, Gao P. SPIN1, negatively regulated by miR-148/152, enhances Adriamycin resistance via upregulating drug metabolizing enzymes and transporter in breast cancer. J Exp Clin Cancer Res. 2018;37:100 pubmed publisher
    ..Mechanistically, drug metabolizing enzymes and transporter CYP2C8, UGT2B4, UGT2B17 and ABCB4 were proven to be downstream effectors of SPIN1...
  7. Francke S, Mamidi R, Solanki B, Scheers E, Jadwin A, Favis R, et al. In vitro metabolism of canagliflozin in human liver, kidney, intestine microsomes, and recombinant uridine diphosphate glucuronosyltransferases (UGT) and the effect of genetic variability of UGT enzymes on the pharmacokinetics of canagliflozin in hum. J Clin Pharmacol. 2015;55:1061-72 pubmed publisher
    ..In vitro incubations with recombinant UGTs revealed involvement of UGT1A9 and UGT2B4 in the formation of M7 and M5, respectively...
  8. Gradinaru J, Romand S, Geiser L, Carrupt P, Spaggiari D, Rudaz S. Inhibition screening method of microsomal UGTs using the cocktail approach. Eur J Pharm Sci. 2015;71:35-45 pubmed publisher
    ..acid for UGT1A3, trifluoperazine for UGT1A4, serotonin for UGT 1A6, isoferulic acid for UGT1A9, codeine for UGT2B4, azidothymidine for UGT2B7, levomedetomidine for UGT2B10, 4-hydroxy-3-methoxymethamphetamine for UGT2B15 and ..
  9. Devineni D, Vaccaro N, Murphy J, Curtin C, Mamidi R, Weiner S, et al. Effects of rifampin, cyclosporine A, and probenecid on the pharmacokinetic profile of canagliflozin, a sodium glucose co-transporter 2 inhibitor, in healthy participants. Int J Clin Pharmacol Ther. 2015;53:115-28 pubmed publisher
    ..of type-2 diabetes mellitus (T2DM), is metabolized by uridine diphosphate-glucuronosyltransferases (UGT) 1A9 and UGT2B4, and is a substrate of P-glycoprotein (P-gp)...

More Information

Publications60

  1. Atsriku C, Hoffmann M, Moghaddam M, Kumar G, Surapaneni S. In vitro metabolism of a novel JNK inhibitor tanzisertib: interspecies differences in oxido-reduction and characterization of enzymes involved in metabolism. Xenobiotica. 2015;45:465-80 pubmed publisher
    ..3. Characterization of UGT isoenzymes in glucuronidation of tanzisertib and CC-418424 revealed that, tanzisertib glucuronide was catalyzed by: UGT1A1, 1A4, 1A10 and 2B4, while CC-418424 glucuronidation was catalyzed by UGT2B4 and 2B7.
  2. Chai J, Feng X, Zhang L, Chen S, Cheng Y, He X, et al. Hepatic expression of detoxification enzymes is decreased in human obstructive cholestasis due to gallstone biliary obstruction. PLoS ONE. 2015;10:e0120055 pubmed publisher
    ..8-fold, and 1.9-fold, respectively (p<0.05). Conversely, the expression levels of liver detoxification enzymes, UGT2B4/7, SULT2A1, GSTA1-4, and GSTM1-4, were reduced by approximately 50% (p<0.05) in human obstructive cholestasis...
  3. Peng Y, Zhang X, Zhu Y, Wu H, Gu S, Chang Q, et al. Atypical Kinetics and Albumin Effect of Glucuronidation of 5-n-Butyl-4-{4-[2-(1H-tetrazole-5- yl)-1H-pyrrol-1-yl]phenylmethyl}-2,4-dihydro-2-(2,6- dichlorophenyl)-3H-1,2,4-triazol-3-one, a Novel Nonpeptide Angiotensin Type 1 Receptor Antagonist, in L. Molecules. 2018;23: pubmed publisher
    ..Five UGTs (UGT1A3, UGT2B4, UGT2B7, UGT1A9 and UGT1A8) were identified that produced abundant Ib monoglucuronide, especially UGT1A3...
  4. Du Z, Cao Y, Li S, Hu C, Fu Z, Huang C, et al. Inhibition of UDP-glucuronosyltransferases (UGTs) by phthalate monoesters. Chemosphere. 2018;197:7-13 pubmed publisher
    ..monoesters exhibited negligible inhibition towards the activity of UGT1A1, UGT1A3, UGT1A6, UGT1A8, UGT1A10, UGT2B4, UGT2B7, UGT2B15 and UGT2B17...
  5. Hanioka N, Kinashi Y, Tanaka Kagawa T, Isobe T, Jinno H. Glucuronidation of mono(2-ethylhexyl) phthalate in humans: roles of hepatic and intestinal UDP-glucuronosyltransferases. Arch Toxicol. 2017;91:689-698 pubmed publisher
    ..Among the recombinant UGTs examined, UGT1A3, UGT1A7, UGT1A8, UGT1A9, UGT1A10, UGT2B4, and UGT2B7 glucuronidated MEHP...
  6. Moscovitz J, Kalgutkar A, Nulick K, Johnson N, Lin Z, Goosen T, et al. Establishing Transcriptional Signatures to Differentiate PXR-, CAR-, and AhR-Mediated Regulation of Drug Metabolism and Transport Genes in Cryopreserved Human Hepatocytes. J Pharmacol Exp Ther. 2018;365:262-271 pubmed publisher
  7. Wijayakumara D, Mackenzie P, McKinnon R, Hu D, Meech R. Regulation of UDP-Glucuronosyltransferases UGT2B4 and UGT2B7 by MicroRNAs in Liver Cancer Cells. J Pharmacol Exp Ther. 2017;361:386-397 pubmed publisher
    The transcriptional regulation of UDP-glucuronosyltransferases UGT2B4 and UGT2B7 has been well studied using liver cancer cell lines, and post-transcriptional regulation of these two UGTs by microRNA (miRNA/miR) miR-..
  8. Wang J, Shidfar A, Ivancic D, Ranjan M, Liu L, Choi M, et al. Overexpression of lipid metabolism genes and PBX1 in the contralateral breasts of women with estrogen receptor-negative breast cancer. Int J Cancer. 2017;140:2484-2497 pubmed publisher
    ..The expression of DHRS2, HMGCS2, UGT2B7, UGT2B11, ALOX15B, HPGD, UGT2B28 and GLYATL1 was significantly higher in ER-negative versus ER-positive CUBs, and ..
  9. Pattanawongsa A, Nair P, Rowland A, Miners J. Human UDP-Glucuronosyltransferase (UGT) 2B10: Validation of Cotinine as a Selective Probe Substrate, Inhibition by UGT Enzyme-Selective Inhibitors and Antidepressant and Antipsychotic Drugs, and Structural Determinants of Enzyme Inhibition. Drug Metab Dispos. 2016;44:378-88 pubmed publisher
    ..Of the UGT enzyme-selective inhibitors employed for reaction phenotyping, only the UGT2B4/7 inhibitor fluconazole reduced recombinant UGT2B10 activity to an appreciable extent...
  10. Devineni D, Polidori D. Clinical Pharmacokinetic, Pharmacodynamic, and Drug-Drug Interaction Profile of Canagliflozin, a Sodium-Glucose Co-transporter 2 Inhibitor. Clin Pharmacokinet. 2015;54:1027-41 pubmed publisher
    ..into two inactive metabolites, M7 and M5 by uridine diphosphate-glucuronosyltransferase (UGT) 1A9 and UGT2B4, respectively...
  11. 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...
  12. Margaillan G, Rouleau M, Klein K, Fallon J, Caron P, Villeneuve L, et al. Multiplexed Targeted Quantitative Proteomics Predicts Hepatic Glucuronidation Potential. Drug Metab Dispos. 2015;43:1331-5 pubmed publisher
    ..abundant UGT in our collection of livers, expressed at 69 pmol/mg microsomal proteins, whereas UGT1A1, UGT1A4, UGT2B4, and UGT2B15 are similarly abundant, averaging 30-34 pmol/mg proteins...
  13. Romand S, Spaggiari D, Marsousi N, Samer C, Desmeules J, Daali Y, et al. Characterization of oxycodone in vitro metabolism by human cytochromes P450 and UDP-glucuronosyltransferases. J Pharm Biomed Anal. 2017;144:129-137 pubmed publisher
    ..produced by UGT2B7 (Km=762±153?M, Vmax=344±20 peak area/min/mg) and to a lesser extent by UGT2B4 (Km=2454±497?M, Vmax=201±19 peak area/min/mg)...
  14. Singh V, Singh L, Vasudevan M, Chattopadhyay I, Borthakar B, Rai A, et al. Esophageal Cancer Epigenomics and Integrome Analysis of Genome-Wide Methylation and Expression in High Risk Northeast Indian Population. OMICS. 2015;19:688-99 pubmed publisher
    ..hypermethylation and downregulation, and 19 genes (SEMG2, CD97, CTNND2, CADM3, OMD, NEFM, FBN2, CTNNB1, DLX6, UGT2B4, CCDC80, PZP, SERPINA4, TNFSF13B, NPC1, COL1A1, TAC3, BMP8A, and IL22RA2) with promoter hypomethylation and ..
  15. Jeong H, Kim J, Lee D, Shim H, Lee H. In Vitro Metabolic Pathways of the New Anti-Diabetic Drug Evogliptin in Human Liver Preparations. Molecules. 2015;20:21802-15 pubmed publisher
    ..of 4(S)-hydroxy-evogliptin (M2) to 4(S)-hydroxyevogliptin glucuronide (M4) was catalyzed by the enzymes UGT2B4 and UGT2B7...
  16. Li X, Zhou Y, Zhou S, Liu H, Xu J, Gao L, et al. Histopathology of melanosis coli and determination of its associated genes by comparative analysis of expression microarrays. Mol Med Rep. 2015;12:5807-15 pubmed publisher
    ..Expression microarray analysis revealed that the significantly downregulated genes were CYP3A4, CYP3A7, UGT2B11 and UGT2B15 in melanosis coli...
  17. Dates C, Fahmi T, Pyrek S, Yao Borengasser A, Borowa Mazgaj B, Bratton S, et al. Human UDP-Glucuronosyltransferases: Effects of altered expression in breast and pancreatic cancer cell lines. Cancer Biol Ther. 2015;16:714-23 pubmed publisher
    ..Expression plasmids for UGT2B isoforms known to glucuronidate cellular lipids, UGT2B4, 2B7, and 2B15 were transfected into MCF-7 and Panc-1 cells, and the cytotoxic effects of these enzymes were ..
  18. Zhao Y, Hou Y, Liu F, Liu A, Jing L, Zhao C, et al. Transcriptome Analysis Reveals that Vitamin A Metabolism in the Liver Affects Feed Efficiency in Pigs. G3 (Bethesda). 2016;6:3615-3624 pubmed publisher
    ..i>CYP2J2, and ANKRD23), and steroid hormone metabolism (CYP1A1, HSD17B2, and UGT2B4) were significantly upregulated in the liver of high-FE pigs...
  19. 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
    ..b>Hyodeoxycholic acid glucuronidation, catalyzed primarily by UGT2B4 and UGT2B7, showed a 7-fold interindividual variation in ..
  20. Jin C, Miners J, Lillywhite K, Mackenzie P. cDNA cloning and expression of two new members of the human liver UDP-glucuronosyltransferase 2B subfamily. Biochem Biophys Res Commun. 1993;194:496-503 pubmed
    Two new UDP-glucuronosyltransferase cDNAs, designated UGT2B10 and UGT2B11, encoding 528 amino acid proteins were isolated from a human liver cDNA library...
  21. Ding Y, Xiong X, Zhou L, Yan S, Qin H, Li H, et al. Preliminary study on Emodin alleviating alpha-naphthylisothiocyanate-induced intrahepatic cholestasis by regulation of liver farnesoid X receptor pathway. Int J Immunopathol Pharmacol. 2016;29:805-811 pubmed
    ..of FXR, small heterodimer partner (SHP), uridine diphosphate glucuronosyltransferase 2 family polypeptide B4 (UGT2B4), and bile salt export pump (BSEP) was detected...
  22. Monaghan G, Clarke D, Povey S, See C, Boxer M, Burchell B. Isolation of a human YAC contig encompassing a cluster of UGT2 genes and its regional localization to chromosome 4q13. Genomics. 1994;23:496-9 pubmed
    Previously we mapped the gene encoding a human bile acid UDP-glucuronosyltransferase (UGT2B4) to chromosome 4...
  23. Kadlubar F, Miller J, Miller E. Hepatic microsomal N-glucuronidation and nucleic acid binding of N-hydroxy arylamines in relation to urinary bladder carcinogenesis. Cancer Res. 1977;37:805-14 pubmed
  24. 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. 'human UGT2B4' and 'mouse Ugt2b5'...
  25. Takekuma Y, Takenaka T, Kiyokawa M, Yamazaki K, Okamoto H, Kitabatake A, et al. Contribution of polymorphisms in UDP-glucuronosyltransferase and CYP2D6 to the individual variation in disposition of carvedilol. J Pharm Pharm Sci. 2006;9:101-12 pubmed
    ..blocking and vasodilating activities, is mainly metabolized by UDP-glucuronosyltransferase (UGT) 1A1, UGT2B4, UGT2B7 and CYP2D6...
  26. Ritter J, Chen F, Sheen Y, Lubet R, Owens I. Two human liver cDNAs encode UDP-glucuronosyltransferases with 2 log differences in activity toward parallel substrates including hyodeoxycholic acid and certain estrogen derivatives. Biochemistry. 1992;31:3409-14 pubmed
    ..Biol. Chem. 266, 7900-7906] have previously been shown to encode isozymes active in the glucuronidation of hyodeoxycholic acid (HDCA) and certain estrogen derivatives (estriols and 3,4-catechol estrogens), respectively...
  27. Babu S, Lakshmi V, Huang G, Zenser T, Davis B. Glucuronide conjugates of 4-aminobiphenyl and its N-hydroxy metabolites. pH stability and synthesis by human and dog liver. Biochem Pharmacol. 1996;51:1679-85 pubmed
    ..Thus, the glucuronide of 4-aminobiphenyl is a major product of dog and human liver slice metabolism and likely to play an important role in the carcinogenic process. ..
  28. Barbier O, Duran Sandoval D, Pineda Torra I, Kosykh V, Fruchart J, Staels B. Peroxisome proliferator-activated receptor alpha induces hepatic expression of the human bile acid glucuronidating UDP-glucuronosyltransferase 2B4 enzyme. J Biol Chem. 2003;278:32852-60 pubmed
    ..Furthermore, treatment of HepG2 cells with Wy 14643 induced the glucuronidation of hyodeoxycholic acid, a specific bile acid UGT2B4 substrate...
  29. Sparks R, Ulrich C, Bigler J, Tworoger S, Yasui Y, Rajan K, et al. UDP-glucuronosyltransferase and sulfotransferase polymorphisms, sex hormone concentrations, and tumor receptor status in breast cancer patients. Breast Cancer Res. 2004;6:R488-98 pubmed
    ..Polymorphic variation in five UGT and SULT genes - UGT1A1 ((TA)6/(TA)7), UGT2B4 (Asp458Glu), UGT2B7 (His268Tyr), UGT2B15 (Asp85Tyr), and SULT1A1 (Arg213His)--may be associated with circulating ..
  30. 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
    ..Of other enzymes displaying activity (UGT1A3, UGT1A9, UGT1A10-H, and UGT2B4), UGT2B4 (CLint,u 0...
  31. 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
    ..inhibition of UGT1A1, UGT1A3, UGT1A8, UGT1A10, UGT2B15, and UGT2B17, and limited inhibition of UGT1A6, UGT1A7 and UGT2B4. However, UGT1A9 was strongly inhibited by PAEs...
  32. Brand W, Boersma M, Bik H, Hoek van den Hil E, Vervoort J, Barron D, et al. Phase II metabolism of hesperetin by individual UDP-glucuronosyltransferases and sulfotransferases and rat and human tissue samples. Drug Metab Dispos. 2010;38:617-25 pubmed publisher
    ..Furthermore, UGT1A6 and UGT2B4 only produce hesperetin 7-O-glucuronide, whereas UGT1A1, UGT1A8, UGT1A9, UGT1A10, UGT2B7, and UGT2B15 conjugate ..
  33. Yong M, Schwartz S, Atkinson C, Makar K, Thomas S, Newton K, et al. Associations between polymorphisms in glucuronidation and sulfation enzymes and mammographic breast density in premenopausal women in the United States. Cancer Epidemiol Biomarkers Prev. 2010;19:537-46 pubmed publisher
    ..07). No associations were observed between polymorphisms in the UGT2B family or SULT1E1 and breast density. Polymorphisms in SULT1A1 and the UGT1A locus may influence percent breast density in premenopausal women. ..
  34. Monaghan G, Burchell B, Boxer M. Structure of the human UGT2B4 gene encoding a bile acid UDP-glucuronosyltransferase. Mamm Genome. 1997;8:692-4 pubmed
  35. Barrett K, Fang H, Cukovic D, Dombkowski A, Kocarek T, Runge Morris M. Upregulation of UGT2B4 Expression by 3'-Phosphoadenosine-5'-Phosphosulfate Synthase Knockdown: Implications for Coordinated Control of Bile Acid Conjugation. Drug Metab Dispos. 2015;43:1061-70 pubmed publisher
    During cholestasis, the bile acid-conjugating enzymes, SULT2A1 and UGT2B4, work in concert to prevent the accumulation of toxic bile acids...
  36. Dura P, Salomon J, Te Morsche R, Roelofs H, Kristinsson J, Wobbes T, et al. High enzyme activity UGT1A1 or low activity UGT1A8 and UGT2B4 genotypes increase esophageal cancer risk. Int J Oncol. 2012;40:1789-96 pubmed publisher
    ..High (OR=0.42; 95% CI, 0.22-0.84) and medium (OR=0.25; 95% CI, 0.12-0.52) activity UGT2B4 genotypes were significantly less often present in ESCC patients...
  37. Gelston E, Coller J, Lopatko O, James H, Schmidt H, White J, et al. Methadone inhibits CYP2D6 and UGT2B7/2B4 in vivo: a study using codeine in methadone- and buprenorphine-maintained subjects. Br J Clin Pharmacol. 2012;73:786-94 pubmed publisher
    To compare the O-demethylation (CYP2D6-mediated), N-demethylation (CYP3A4-mediated) and 6-glucuronidation (UGT2B4/7-mediated) metabolism of codeine between methadone- and buprenorphine-maintained CYP2D6 extensive metabolizer subjects...
  38. Sun C, Huo D, Southard C, Nemesure B, Hennis A, Cristina Leske M, et al. A signature of balancing selection in the region upstream to the human UGT2B4 gene and implications for breast cancer risk. Hum Genet. 2011;130:767-75 pubmed publisher
    UDP-glucuronosyltransferase 2 family, polypeptide B4 (UGT2B4) is an important metabolizing enzyme involved in the clearance of many xenobiotics and endogenous substrates, especially steroid hormones and bile acids...
  39. 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
    ..Therefore, UGT1A9 is likely to be the most important enzyme in the glucuronidation of both substrates as this enzyme had the lowest K(m) and is expressed in both the intestine and at high levels in the liver...
  40. Levesque E, Menard V, Laverdière I, Bellemare J, Barbier O, Girard H, et al. Extensive splicing of transcripts encoding the bile acid-conjugating enzyme UGT2B4 modulates glucuronidation. Pharmacogenet Genomics. 2010;20:195-210 pubmed publisher
    b>UGT2B4 is a member of the UDP-glucuronosyltransferase (UGT) superfamily, a major detoxifying system in humans. UGT2B4 is involved in bile acids metabolism and highly expressed in liver and extrahepatic tissues...
  41. Barre L, Fournel Gigleux S, Finel M, Netter P, Magdalou J, Ouzzine M. Substrate specificity of the human UDP-glucuronosyltransferase UGT2B4 and UGT2B7. Identification of a critical aromatic amino acid residue at position 33. FEBS J. 2007;274:1256-64 pubmed
    ..present distinct but overlapping substrate specificity, sharing common substrates such as the bile acid hyodeoxycholic acid (HDCA) and catechol-estrogens...
  42. Katz D, Carr R, Grimm D, Xiong H, Holley Shanks R, Mueller T, et al. Organic anion transporting polypeptide 1B1 activity classified by SLCO1B1 genotype influences atrasentan pharmacokinetics. Clin Pharmacol Ther. 2006;79:186-96 pubmed
    ..Genotypes for cytochrome P450 3A5, uridine diphosphate-glucuronosyltransferase (UGT) 1A1, UGT2B4, UGT2B15, adenosine triphosphate-binding cassette subfamily B (ABCB) 1, solute carrier organic anion transporter (..
  43. Saeki M, Saito Y, Jinno H, Tanaka Kagawa T, Ohno A, Ozawa S, et al. Single nucleotide polymorphisms and haplotype frequencies of UGT2B4 and UGT2B7 in a Japanese population. Drug Metab Dispos. 2004;32:1048-54 pubmed
    Both UDP-glucuronosyltransferase 2B4 (UGT2B4) and UGT2B7 are expressed mainly in the human liver and have several overlapping substrates; e.g., catechol estrogens, bile acids, codeine, and carvedilol...
  44. Joseph T, Wang S, Liu X, Kulkarni K, Wang J, Xu H, et al. Disposition of flavonoids via enteric recycling: enzyme stability affects characterization of prunetin glucuronidation across species, organs, and UGT isoforms. Mol Pharm. 2007;4:883-94 pubmed
    ..In conclusion, prunetin glucuronidation is species-, organ-, and UGT-isoform-dependent, all of which may be impacted by the thermostability of specific UGT isoforms involved in the metabolism. ..
  45. 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
    ..001) and UGT2B10 (P = 0.0018) mRNA levels in HuH-7 cells and UGT2B4 (P < 0.001) and UGT2B10 (P = 0.018) mRNA in Hep3B cells...
  46. Berkhout M, Roelofs H, te Morsche R, Dekker E, van Krieken J, Nagengast F, et al. Detoxification enzyme polymorphisms are not involved in duodenal adenomatosis in familial adenomatous polyposis. Br J Surg. 2008;95:499-505 pubmed
    ..glucuronosyltransferases (UGTs) and glutathione S-transferases (GSTs): UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A10, UGT2B4, UGT2B7, UGT2B15, GSTA1, GSTP1, GSTM1 and GSTT1...
  47. Yermachenko A, Dvornyk V. UGT2B4 previously implicated in the risk of breast cancer is associated with menarche timing in Ukrainian females. Gene. 2016;590:85-9 pubmed publisher
    ..SNP rs13111134 located in UGT2B4 showed the most significant association with AAM (0.431years per allele A, padj=0...
  48. Jackson M, McCarthy L, Harding D, Wilson S, Coughtrie M, Burchell B. Cloning of a human liver microsomal UDP-glucuronosyltransferase cDNA. Biochem J. 1987;242:581-8 pubmed
    ..The possible site of translation initiation of this sequence is discussed with reference to a rat UDP-glucuronosyltransferase cDNA clone (RLUG 38). ..
  49. Barbier O, Torra I, Sirvent A, Claudel T, Blanquart C, Duran Sandoval D, et al. FXR induces the UGT2B4 enzyme in hepatocytes: a potential mechanism of negative feedback control of FXR activity. Gastroenterology. 2003;124:1926-40 pubmed
    ..The human uridine 5'-diphosphate-glucuronosyltransferase 2B4 (UGT2B4) converts hydrophobic bile acids into more hydrophilic glucuronide derivatives...
  50. King C, Rios G, Assouline J, Tephly T. Expression of UDP-glucuronosyltransferases (UGTs) 2B7 and 1A6 in the human brain and identification of 5-hydroxytryptamine as a substrate. Arch Biochem Biophys. 1999;365:156-62 pubmed
    ..UGT1A6 could play an important role in the glucuronidation of 5-hydroxytryptamine in vivo, therefore terminating the actions of the neurotransmitter. ..
  51. Fournel Gigleux S, Jackson M, Wooster R, Burchell B. Expression of a human liver cDNA encoding a UDP-glucuronosyltransferase catalysing the glucuronidation of hyodeoxycholic acid in cell culture. FEBS Lett. 1989;243:119-22 pubmed
    ..This expressed UDPGT glycoprotein catalysed the glucuronidation of hyodeoxycholic acid forming an ether glucuronide...