TY - JOUR
T1 - The inherited deficiency of hepatic UDP-glucuronyltransferase
T2 - Structure-activity relationships of in vitro stimulators
AU - Lalani, El Nasir M.A.
AU - Weatherill, Philip J.
AU - Kennedy, Sue M.E.
AU - Burchell, Brian
PY - 1980
Y1 - 1980
N2 - More than 18 compounds have been tested for their ability to stimulate defective UDP-glucuronyltransferase activity of Gunn rat liver homogenates towards 2-aminophenol, up to levels of transferase activity in similarly treated Wistar rat liver homogenates. The minimum structural requirements of an effective compound are a combination of the presence of an electron-attracting atom or group and a sparing solubility in water. The activation of defective UDP-glucuronyltransferase towards 2-aminophenol by pentan-3-one is reversible. The possible mechanism of action of alkyl ketone activators is discussed.
AB - More than 18 compounds have been tested for their ability to stimulate defective UDP-glucuronyltransferase activity of Gunn rat liver homogenates towards 2-aminophenol, up to levels of transferase activity in similarly treated Wistar rat liver homogenates. The minimum structural requirements of an effective compound are a combination of the presence of an electron-attracting atom or group and a sparing solubility in water. The activation of defective UDP-glucuronyltransferase towards 2-aminophenol by pentan-3-one is reversible. The possible mechanism of action of alkyl ketone activators is discussed.
UR - http://www.scopus.com/inward/record.url?scp=0018905885&partnerID=8YFLogxK
U2 - 10.1016/0006-2952(80)90271-3
DO - 10.1016/0006-2952(80)90271-3
M3 - Article
C2 - 6775636
AN - SCOPUS:0018905885
SN - 0006-2952
VL - 29
SP - 2367
EP - 2371
JO - Biochemical Pharmacology
JF - Biochemical Pharmacology
IS - 17
ER -