UDP-glucuronosyltransferase 1-3 is an enzyme that in humans is encoded by the UGT1A3 gene.[5][6][7]
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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.[8][9][10]
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- Tukey RH, Strassburg CP (2000). "Human UDP-glucuronosyltransferases: metabolism, expression, and disease". Annual Review of Pharmacology and Toxicology. 40: 581–616. doi:10.1146/annurev.pharmtox.40.1.581. PMID 10836148.
- Tukey RH, Strassburg CP (March 2001). "Genetic multiplicity of the human UDP-glucuronosyltransferases and regulation in the gastrointestinal tract". Molecular Pharmacology. 59 (3): 405–14. doi:10.1124/mol.59.3.405. PMID 11179432. S2CID 21500183.
- King CD, Rios GR, Green MD, Tephly TR (September 2000). "UDP-glucuronosyltransferases". Current Drug Metabolism. 1 (2): 143–61. doi:10.2174/1389200003339171. PMID 11465080.
- Moghrabi N, Sutherland L, Wooster R, Povey S, Boxer M, Burchell B (May 1992). "Chromosomal assignment of human phenol and bilirubin UDP-glucuronosyltransferase genes (UGT1A-subfamily)". Annals of Human Genetics. 56 (2): 81–91. doi:10.1111/j.1469-1809.1992.tb01134.x. PMID 1503396. S2CID 40140345.
- Mojarrabi B, Butler R, Mackenzie PI (August 1996). "cDNA cloning and characterization of the human UDP glucuronosyltransferase, UGT1A3". Biochemical and Biophysical Research Communications. 225 (3): 785–90. doi:10.1006/bbrc.1996.1251. PMID 8780690.
- Strassburg CP, Manns MP, Tukey RH (July 1997). "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. PMID 9230212.
- Strassburg CP, Oldhafer K, Manns MP, Tukey RH (August 1997). "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. doi:10.1124/mol.52.2.212. PMID 9271343. S2CID 37098463.
- Strassburg CP, Manns MP, Tukey RH (April 1998). "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. doi:10.1074/jbc.273.15.8719. PMID 9535849.
- Green MD, King CD, Mojarrabi B, Mackenzie PI, Tephly TR (June 1998). "Glucuronidation of amines and other xenobiotics catalyzed by expressed human UDP-glucuronosyltransferase 1A3". Drug Metabolism and Disposition. 26 (6): 507–12. PMID 9616184.
- Strassburg CP, Kneip S, Topp J, Obermayer-Straub P, Barut A, Tukey RH, Manns MP (November 2000). "Polymorphic gene regulation and interindividual variation of UDP-glucuronosyltransferase activity in human small intestine". The Journal of Biological Chemistry. 275 (46): 36164–71. doi:10.1074/jbc.M002180200. PMID 10748067.
- Barbier O, Albert C, Martineau I, Vallée M, High K, Labrie F, Hum DW, Labrie C, Bélanger A (March 2001). "Glucuronidation of the nonsteroidal antiestrogen EM-652 (SCH 57068), by human and monkey steroid conjugating UDP-glucuronosyltransferase enzymes". Molecular Pharmacology. 59 (3): 636–45. doi:10.1124/mol.59.3.636. PMID 11179460. S2CID 38640331.
- Turgeon D, Chouinard S, Belanger P, Picard S, Labbe JF, Borgeat P, Belanger A (June 2003). "Glucuronidation of arachidonic and linoleic acid metabolites by human UDP-glucuronosyltransferases". Journal of Lipid Research. 44 (6): 1182–91. doi:10.1194/jlr.M300010-JLR200. PMID 12639971.
- Zhang JY, Zhan J, Cook CS, Ings RM, Breau AP (May 2003). "Involvement of human UGT2B7 and 2B15 in rofecoxib metabolism". Drug Metabolism and Disposition. 31 (5): 652–8. doi:10.1124/dmd.31.5.652. PMID 12695355. S2CID 23434477.