Characterisation of glucuronidation and transport in V79 cells co-expressing UGT1A1 and MRP1.
The co-ordinated glucuronidation and export of compounds from cells is an important determinant in the detoxification of many compounds in vivo. Many UDP-glucuronosyltransferases (UGTs) and several multidrug resistance proteins (MRPs) have been cloned and individually expressed to assess specificity of glucuronidation and transport. However, to further understand the interplay between glucuronidation and transport we are developing stable cell lines that express different combinations of UGT and MRP isoforms. V79 cells expressing both UGT1A1 and MRP1 have been established. The ability of these cell lines to both glucuronidate and transport compounds was assessed ex vivo using estradiol and bilirubin as substrates.
Cuff
R L
RL
Department of Molecular and Cellular Pathology, Ninewells Hospital and Medical School, University of Dundee, Scotland DD1 9SY, Dundee, UK.
Wade
L T
LT
Rychlik
B
B
Jedlitschky
G A
GA
Burchell
B
B
D018528:ATP-Binding Cassette Transporters / Q000032:analysis / Q000502:physiology*; D000818:Animals; D001663:Bilirubin / Q000378:metabolism; D001692:Biological Transport; D002460:Cell Line; D004958:Estradiol / Q000378:metabolism; D020719:Glucuronides / Q000378:metabolism; D014453:Glucuronosyltransferase / Q000032:analysis / Q000502:physiology*; D027425:ATP-Binding Cassette, Sub-Family C Proteins
D018528:ATP-Binding Cassette Transporters; D001663:Bilirubin; D004958:Estradiol; D020719:Glucuronides; D014453:Glucuronosyltransferase; D027425:ATP-Binding Cassette, Sub-Family C Proteins