Glucuronidation of retinoids by rat recombinant UDP: glucuronosyltransferase 1.1 (bilirubin UGT)

Drug Metab Dispos. 1997 Jul;25(7):889-92.

Abstract

Rat liver recombinant BR1UGT1.1 was found to have significant activity toward retinoid substrates. UGT1.1 glucuronidation activity was 91 +/- 18 pmol/mg x min for atRA and 113 +/- 19 pmol/mg x min for 5,6-epoxy-atRA. The apparent K(M) and V(max) of atRA acid glucuronidation by UGT1.1 were 59.1 +/- 5.4 microM and 158 +/- 43 pmol/mg x min, respectively. SDS-PAGE and Western blot analysis of UGT1.1-transfected HK293 membrane proteins photolabeled with [11,12-3H]atRA revealed a protein of approximately 56 kDa that was labeled by [3H]atRA, detected by anti-pNP UGT antibody and not present in membranes from nontransfected HK293 cells. Liver microsomes from Gunn rats, which lack UGT1.1, had significant activity toward atRA (111 +/- 28 pmol/mg x min).

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Affinity Labels
  • Animals
  • Blotting, Western
  • Electrophoresis, Polyacrylamide Gel
  • Glucuronates / metabolism
  • Glucuronosyltransferase / metabolism*
  • Humans
  • Isoenzymes / metabolism*
  • Kinetics
  • Microsomes, Liver / enzymology
  • Precipitin Tests
  • Rats
  • Rats, Gunn
  • Rats, Sprague-Dawley
  • Rats, Wistar
  • Recombinant Proteins / metabolism
  • Retinoids / metabolism*
  • Substrate Specificity

Substances

  • Affinity Labels
  • Glucuronates
  • Isoenzymes
  • Recombinant Proteins
  • Retinoids
  • Glucuronosyltransferase