Corning® Supersomes™ Human UGT1A6, 0.5 enzyme prepared from insect cells infected with baculovirus containing human UGT1A6 cDNAs
UDP-glucuronosyltransferases (UGT) represent the major phase II drug metabolism pathway in human. UGT enzymes catalyze the transfer of glucuronic acid (derived from UDPGA co-factor) to xenobiotics and endogenous substrates having nucleophilic acceptor groups, making them more polar and readily excreted in urine or bile. To date, at least 18 human UGT enzymes have been cloned and sequenced. Like the P450 enzymes, UGTs possess broad and overlapping substrate specificities. Clinically relevant drug interactions have been identified for UGT isoforms, leading regulatory agencies (FDA) to require drug interaction testing for compounds showing significant UGT metabolism.
UGT1A6 is a phenol-metabolizing UGT, primarily involved in the glucuronidation of simple phenols and planar arylamines that mediates the conjugation of many currently prescribed drugs including antidepressants, neuroleptics and ß-adrenoreceptor blockers. UGT1A6 is expressed in liver and intestine. Selective substrates include serotonin, the serotonin metabolite 5-hydroxytryptophol and desferipone.