Characterization of a new class of inhibitors of the recombinant human liver UDP-glucuronosyltransferase, UGT16

• Published in: Biochimica et biophysica acta Vol. 1243; no. 1; pp. 9 - 14
• Main Author: Battaglia, E
• Format: Journal Article
• Language: English
• Published: Netherlands 18.01.1995
• Subjects: Binding Sites; Computer Simulation; Deoxyuridine - analogs & derivatives; Deoxyuridine - pharmacology; Dose-Response Relationship, Drug; Glucuronosyltransferase - antagonists & inhibitors; Humans; Hymecromone - metabolism; Isoenzymes - antagonists & inhibitors; Kinetics; Liver - enzymology; Models, Molecular; Naphthols - metabolism; Propanolamines - pharmacology; Recombinant Proteins - antagonists & inhibitors; Sulfones - pharmacology; Uridine - analogs & derivatives; Uridine - pharmacology

The inhibitory effect of a series of novel structurally related compounds on the human UDP-glucuronosyltransferase UGT1*6 stably expressed in a V79 cell line was investigated. The inhibitors contain a lipophilic N-acyl phenylaminoalcohol residue and a uridine moiety connected by a spacer varying for...