Biology:UGT1A3

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Generic protein structure example

UDP-glucuronosyltransferase 1-3 is an enzyme that in humans is encoded by the UGT1A3 gene.[1][2][3]

This gene encodes a UDP-glucuronosyltransferase, an enzyme of the glucuronidation pathway that transforms small lipophilic molecules, such as steroids, bilirubin, hormones, and drugs, into water-soluble, excretable metabolites. This gene is part of a complex locus that encodes several UDP-glucuronosyltransferases. The locus includes thirteen unique alternate first exons followed by four common exons. Four of the alternate first exons are considered pseudogenes. Each of the remaining nine 5' exons may be spliced to the four common exons, resulting in nine proteins with different N-termini and identical C-termini. Each first exon encodes the substrate binding site, and is regulated by its own promoter. Substrates of this enzyme include estrone, 2-hydroxyestrone, and metabolites of benzo(a)pyrene.[4][5][6]

References

  1. "Gene: UGT1A3 (ENSG00000243135) - Summary - Homo sapiens - Ensembl genome browser 89". http://may2017.archive.ensembl.org/Homo_sapiens/Gene/Summary?db=core;g=ENSG00000243135;r=2:233729108-233773299;t=ENST00000482026. 
  2. "Gene: Ugt1a2 (ENSMUSG00000090171) - Summary - Mus musculus - Ensembl genome browser 89". http://may2017.archive.ensembl.org/Mus_musculus/Gene/Summary?db=core;g=ENSMUSG00000090171;r=1:88200601-88218997;t=ENSMUST00000049289. 
  3. "The UDP glycosyltransferase gene superfamily: recommended nomenclature update based on evolutionary divergence". Pharmacogenetics 7 (4): 255–69. August 1997. doi:10.1097/00008571-199708000-00001. PMID 9295054. 
  4. "A novel complex locus UGT1 encodes human bilirubin, phenol, and other UDP-glucuronosyltransferase isozymes with identical carboxyl termini". The Journal of Biological Chemistry 267 (5): 3257–61. February 1992. doi:10.1016/S0021-9258(19)50724-4. PMID 1339448. 
  5. "Thirteen UDPglucuronosyltransferase genes are encoded at the human UGT1 gene complex locus". Pharmacogenetics 11 (4): 357–68. June 2001. doi:10.1097/00008571-200106000-00011. PMID 11434514. 
  6. "UGT1A3 UDP glucuronosyltransferase family 1 member A3 [Homo sapiens (human) - Gene - NCBI"]. https://www.ncbi.nlm.nih.gov/gene?Db=gene&Cmd=ShowDetailView&TermToSearch=54659. 

Further reading

  • "Human UDP-glucuronosyltransferases: metabolism, expression, and disease". Annual Review of Pharmacology and Toxicology 40: 581–616. 2000. doi:10.1146/annurev.pharmtox.40.1.581. PMID 10836148. 
  • "Genetic multiplicity of the human UDP-glucuronosyltransferases and regulation in the gastrointestinal tract". Molecular Pharmacology 59 (3): 405–14. March 2001. doi:10.1124/mol.59.3.405. PMID 11179432. 
  • "UDP-glucuronosyltransferases". Current Drug Metabolism 1 (2): 143–61. September 2000. doi:10.2174/1389200003339171. PMID 11465080. 
  • "Chromosomal assignment of human phenol and bilirubin UDP-glucuronosyltransferase genes (UGT1A-subfamily)". Annals of Human Genetics 56 (2): 81–91. May 1992. doi:10.1111/j.1469-1809.1992.tb01134.x. PMID 1503396. 
  • "cDNA cloning and characterization of the human UDP glucuronosyltransferase, UGT1A3". Biochemical and Biophysical Research Communications 225 (3): 785–90. August 1996. doi:10.1006/bbrc.1996.1251. PMID 8780690. 
  • "Differential down-regulation of the UDP-glucuronosyltransferase 1A locus is an early event in human liver and biliary cancer". Cancer Research 57 (14): 2979–85. July 1997. PMID 9230212. 
  • "Differential expression of the UGT1A locus in human liver, biliary, and gastric tissue: identification of UGT1A7 and UGT1A10 transcripts in extrahepatic tissue". Molecular Pharmacology 52 (2): 212–20. August 1997. doi:10.1124/mol.52.2.212. PMID 9271343. 
  • "Expression of the UDP-glucuronosyltransferase 1A locus in human colon. Identification and characterization of the novel extrahepatic UGT1A8". The Journal of Biological Chemistry 273 (15): 8719–26. April 1998. doi:10.1074/jbc.273.15.8719. PMID 9535849. 
  • "Glucuronidation of amines and other xenobiotics catalyzed by expressed human UDP-glucuronosyltransferase 1A3". Drug Metabolism and Disposition 26 (6): 507–12. June 1998. PMID 9616184. 
  • "Polymorphic gene regulation and interindividual variation of UDP-glucuronosyltransferase activity in human small intestine". The Journal of Biological Chemistry 275 (46): 36164–71. November 2000. doi:10.1074/jbc.M002180200. PMID 10748067. 
  • "Glucuronidation of the nonsteroidal antiestrogen EM-652 (SCH 57068), by human and monkey steroid conjugating UDP-glucuronosyltransferase enzymes". Molecular Pharmacology 59 (3): 636–45. March 2001. doi:10.1124/mol.59.3.636. PMID 11179460. 
  • "Glucuronidation of arachidonic and linoleic acid metabolites by human UDP-glucuronosyltransferases". Journal of Lipid Research 44 (6): 1182–91. June 2003. doi:10.1194/jlr.M300010-JLR200. PMID 12639971. 
  • "Involvement of human UGT2B7 and 2B15 in rofecoxib metabolism". Drug Metabolism and Disposition 31 (5): 652–8. May 2003. doi:10.1124/dmd.31.5.652. PMID 12695355.