1P-02 PDF
Effects of Low UDP-glucuronosyltransferase 1A1 Activity on Metabolism of Bilirubin and Acetaminophen
UDP-glucuronosyltransferase 1A1 (UGT1A1), a member enzyme of UGT1A subfamily, catalyzes glucuronidation of many kinds of drugs besides bilirubin. As UGT1A1 is a main glucuronidation enzyme of bilirubin, the mutation in the UGT1A1 gene causes hyperbilirubinemia. Bilirubin has two sites capable of glucuronidation and forms bilirubin mono- and di-glucuronides (BMG and BDG). Acetaminophen is metabolized to acetaminophen glucuronide. The activity of muted UGT1A1 enzyme using bilirubin and acetaminophen as substrates was evaluated in UGT1A1-expression cells.