TABLE 1

Previous studies that described the enzyme kinetic mechanism of UGT enzymes

Enzyme SourceAglycone SubstrateReaction MechanismReference
Guinea pig liver microsomesBilirubinCompulsory-order ternary complex (UDPGA first, aglycone second) or iso-Theorell-ChancePotrepka and Spratt, 1972
Beef and guinea pig liver microsomesp-NitrophenolRapid equilibrium random-order ternary complexVessey and Zakim, 1972
Rat liver microsomesMorphineCompulsory-order ternary complex (UDPGA first, aglycone second)Sanchez and Tephly, 1975
Pig kidney microsomesEstroneTernary-complex mechanism, iso-Theorell-Chance (aglycone first, UDPGA second)Rao et al., 1976
Purified UGT from rat liverChenodeoxycholic acid and testosteroneTernary-complex mechanismMatern et al., 1982
Rat intestinal microsomes1-NaphtholCompulsory-order ternary complex (aglycone first, UDPGA second)Koster and Noordhoek, 1983
Two purified UGTs from rat liverAndrosterone and testosteroneRapid equilibrium random-order ternary complexFalany et al., 1987
Purified UGT from human liverHyodeoxycholic acidTernary-complex mechanismMatern et al., 1991
Purified UGT from rat liver microsomesSubstituted phenolsRandom-order ternary complexYin et al., 1994
Recombinant human UGTs from 1A familyEntacapone, scopoletin, umbelliferone, 1-naphthol, 4-hydroxyestrone, ethinylestradiolCompulsory-order ternary complex (UDPGA first, aglycone second)Luukkanen et al., 2005
Recombinant human UGT1A6ScopoletinCompulsory-order ternary complex (UDPGA first, aglycone second)Patana et al., 2007