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Gene Review

UGT1A3  -  UDP glucuronosyltransferase 1 family,...

Homo sapiens

Synonyms: GNT1, UDP-glucuronosyltransferase 1-3, UDP-glucuronosyltransferase 1-C, UDP-glucuronosyltransferase 1A3, UDPGT, ...
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High impact information on UGT1A3


Biological context of UGT1A3


Anatomical context of UGT1A3


Associations of UGT1A3 with chemical compounds

  • None of the UGTs examined catalyzed the N-glucuronidation of S(-)-nicotine, R(+)-nicotine, and S(-)-cotinine, including UGT1A3 and UGT1A4, the only isoforms known to catalyze many substrates at a tertiary amine [15].
  • UGT1A3 also catalyzed the glucuronidation of the previously investigated 1-phenylimidazole but none of the newly investigated compounds [16].
  • Cotinine glucuronidation by either UGT1A3 or UGT1A9 was not detected [17].
  • Kinetic analysis showed that UGT2B7 exhibits much higher glucuronidation efficiency (Vmax/Km) with ibuprofen, ketoprofen, and others, compared to UGT1A3 [18].
  • Despite being a poor substrate with UGT1A3, coumarin-3-carboxylic acid was not a substrate for any other UGT isoform tested in this study, suggesting that it could be a specific substrate for UGT1A3 [18].
  • This study did not investigate genotype-phenotype association, but raise the possibility that genetically determined variation might contribute to variability in the inactivation of estrone by UGT1A3 and subsequent changes in lifetime exposure to estrogens potentially modifying risk of cancer [19].
  • UDCA does not induce UGT1A3 transcription [20].

Other interactions of UGT1A3

  • Several human UDP-glucuronosyltransferases (UGTs) have been shown to catalyze the formation of acyl-glucuronides, including UGT2B7, UGT1A3, and UGT1A9 [18].
  • Human recombinant UGT1A3, 1A9, 1A10 and 2B7 were actively involved in the glucuronidation of all NSAIDs while UGT1A7 and the intestine-specific UGT1A8 had no glucuronidating activity towards those compounds [21].
  • UGT1A1 had the highest Vmax followed by UGT1A3 [12].
  • The results from this study demonstrated that the in vitro formation of 3-hydroxydesloratadine-glucuronide from 3-hydroxydesloratadine was mediated via UGT1A1, UGT1A3 and UGT2B15 in human liver [22].
  • To this end, we have isolated the UGT1A3, UGT1A4, and UGT1A5 proximal promoters and begun to investigate the regulatory elements necessary for activity in vitro [9].

Analytical, diagnostic and therapeutic context of UGT1A3

  • The cDNA encoding the UDP glucuronosyltransferase, UGT1A3, has been cloned and expressed in cell culture [11].
  • The glucuronidation activity of UGT1A3 was determined by reverse phase-high performance liquid chromatography (RP-HPLC) coupled with a diode array detector (DAD) [23].
  • METHODS: The full-length UGT1A3 gene was amplified by reverse transcription-polymerase chain reaction (RT-PCR) using total RNA from human liver as template [23].
  • Glucuronidation assay and HPLC analysis indicated UGT1A3 expressed heterologously in CHL cells was in an active form, and one of the gulcuronides corresponding to quercetin was also detected [23].


  1. The liver X-receptor alpha controls hepatic expression of the human bile acid-glucuronidating UGT1A3 enzyme in human cells and transgenic mice. Verreault, M., Senekeo-Effenberger, K., Trottier, J., Bonzo, J.A., Bélanger, J., Kaeding, J., Staels, B., Caron, P., Tukey, R.H., Barbier, O. Hepatology (2006) [Pubmed]
  2. Human UDP-glucuronosyltransferase (UGT)1A3 enzyme conjugates chenodeoxycholic acid in the liver. Trottier, J., Verreault, M., Grepper, S., Mont??, D., B??langer, J., Kaeding, J., Caron, P., Inaba, T.T., Barbier, O. Hepatology (2006) [Pubmed]
  3. Variation of hepatic glucuronidation: Novel functional polymorphisms of the UDP-glucuronosyltransferase UGT1A4. Ehmer, U., Vogel, A., Schütte, J.K., Krone, B., Manns, M.P., Strassburg, C.P. Hepatology (2004) [Pubmed]
  4. Gastrointestinally distributed UDP-glucuronosyltransferase 1A10, which metabolizes estrogens and nonsteroidal anti-inflammatory drugs, depends upon phosphorylation. Basu, N.K., Kubota, S., Meselhy, M.R., Ciotti, M., Chowdhury, B., Hartori, M., Owens, I.S. J. Biol. Chem. (2004) [Pubmed]
  5. Glucuronidation of amines and other xenobiotics catalyzed by expressed human UDP-glucuronosyltransferase 1A3. Green, M.D., King, C.D., Mojarrabi, B., Mackenzie, P.I., Tephly, T.R. Drug Metab. Dispos. (1998) [Pubmed]
  6. Development of an assay using 4-trifluoromethylumbelliferyl as a marker substrate for assessment of drug-drug interactions to multiple isoforms of UDP-glucuronosyltransferases. Baranczewski, P., Kallin, A., Andersson, A., Hagigi, S., Aberg, M., Postlind, H., Mankowitz, L. Assay and drug development technologies. (2004) [Pubmed]
  7. Genetic variants of human UGT1A3: functional characterization and frequency distribution in a Chinese Han population. Chen, Y., Chen, S., Li, X., Wang, X., Zeng, S. Drug Metab. Dispos. (2006) [Pubmed]
  8. Glucuronidation of catechol estrogens by expressed human UDP-glucuronosyltransferases (UGTs) 1A1, 1A3, and 2B7. Cheng, Z., Rios, G.R., King, C.D., Coffman, B.L., Green, M.D., Mojarrabi, B., Mackenzie, P.I., Tephly, T.R. Toxicol. Sci. (1998) [Pubmed]
  9. Isolation of the UDP-Glucuronosyltransferase 1A3 and 1A4 Proximal Promoters and Characterization of Their Dependence on the Transcription Factor Hepatocyte Nuclear Factor 1{alpha}. Gardner-Stephen, D.A., Mackenzie, P.I. Drug Metab. Dispos. (2007) [Pubmed]
  10. Inactivation of the pure antiestrogen fulvestrant and other synthetic estrogen molecules by UDP-glucuronosyltransferase 1A enzymes expressed in breast tissue. Chouinard, S., Tessier, M., Vernouillet, G., Gauthier, S., Labrie, F., Barbier, O., Bélanger, A. Mol. Pharmacol. (2006) [Pubmed]
  11. cDNA cloning and characterization of the human UDP glucuronosyltransferase, UGT1A3. Mojarrabi, B., Butler, R., Mackenzie, P.I. Biochem. Biophys. Res. Commun. (1996) [Pubmed]
  12. Human liver UDP-glucuronosyltransferase isoforms involved in the glucuronidation of 7-ethyl-10-hydroxycamptothecin. Hanioka, N., Ozawa, S., Jinno, H., Ando, M., Saito, Y., Sawada, J. Xenobiotica (2001) [Pubmed]
  13. Characterization of afloqualone N-glucuronidation: species differences and identification of human UDP-glucuronosyltransferase isoform(s). Kaji, H., Kume, T. Drug Metab. Dispos. (2005) [Pubmed]
  14. Comparative N-glucuronidation kinetics of ketotifen and amitriptyline by expressed human UDP-glucuronosyltransferases and liver microsomes. Breyer-Pfaff, U., Mey, U., Green, M.D., Tephly, T.R. Drug Metab. Dispos. (2000) [Pubmed]
  15. N-glucuronidation of nicotine and cotinine in human: formation of cotinine glucuronide in liver microsomes and lack of catalysis by 10 examined UDP-glucuronosyltransferases. Ghosheh, O., Hawes, E.M. Drug Metab. Dispos. (2002) [Pubmed]
  16. Quaternary ammonium-linked glucuronidation of 1-substituted imidazoles: studies of human UDP-glucuronosyltransferases involved and substrate specificities. Vashishtha, S.C., Hawes, E.M., McKay, G., McCann, D.J. Drug Metab. Dispos. (2001) [Pubmed]
  17. N-glucuronidation of nicotine and cotinine by human liver microsomes and heterologously expressed UDP-glucuronosyltransferases. Kuehl, G.E., Murphy, S.E. Drug Metab. Dispos. (2003) [Pubmed]
  18. Glucuronidation of carboxylic acid containing compounds by UDP-glucuronosyltransferase isoforms. Sakaguchi, K., Green, M., Stock, N., Reger, T.S., Zunic, J., King, C. Arch. Biochem. Biophys. (2004) [Pubmed]
  19. A pharmacogenomics study of the human estrogen glucuronosyltransferase UGT1A3. Caillier, B., Lépine, J., Tojcic, J., Ménard, V., Perusse, L., Bélanger, A., Barbier, O., Guillemette, C. Pharmacogenet. Genomics (2007) [Pubmed]
  20. Regulation of the human bile acid UDP-glucuronosyltransferase 1A3 by the farnesoid X receptor and bile acids. Erichsen, T.J., Aehlen, A., Ehmer, U., Kalthoff, S., Manns, M.P., Strassburg, C.P. J. Hepatol. (2010) [Pubmed]
  21. Carboxyl nonsteroidal anti-inflammatory drugs are efficiently glucuronidated by microsomes of the human gastrointestinal tract. Sabolovic, N., Heydel, J.M., Li, X., Little, J.M., Humbert, A.C., Radominska-Pandya, A., Magdalou, J. Biochim. Biophys. Acta (2004) [Pubmed]
  22. Identification of human UDP-glucuronosyltransferase enzyme(s) responsible for the glucuronidation of 3-hydroxydesloratadine. Ghosal, A., Yuan, Y., Hapangama, N., Su, A.D., Alvarez, N., Chowdhury, S.K., Alton, K.B., Patrick, J.E., Zbaida, S. Biopharmaceutics & drug disposition. (2004) [Pubmed]
  23. Heterologous expression of active human uridine diphosphate glucuronosyltransferase 1A3 in Chinese hamster lung cells. Chen, Y.K., Li, X., Chen, S.Q., Zeng, S. World J. Gastroenterol. (2005) [Pubmed]
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