UDP-glucuronosyltransferase 1-3 is an enzyme that in humans is encoded by the UGT1A3gene.[5][6][7]
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]
^Mackenzie PI, Owens IS, Burchell B, Bock KW, Bairoch A, Bélanger A, et al. (August 1997). "The UDP glycosyltransferase gene superfamily: recommended nomenclature update based on evolutionary divergence". Pharmacogenetics. 7 (4): 255–69. doi:10.1097/00008571-199708000-00001. PMID9295054.
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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. PMID9230212.
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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. PMID9616184.
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. PMID11179460. S2CID38640331.
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. PMID12695355. S2CID23434477.
