The dominant sex hormone testosterone is mainly metabolized by liver enzymes belonging to the uridine-diphospho (UDP) glucuronosyltransferase (UGT) family. These are main phase II enzymes, and they have an important role in detoxification of endogenous exogenous compounds humans. aim present study was improve understanding binding properties UGT2B17. A homology modelling procedure used generate...

Background: Infertility is a common condition affecting approximately 10–20% of the reproductive age population. Idiopathic infertility cases are thought to have genetic basis, but underlying causes largely unknown. However, basis male in humans only partially understood. The Purpose study understand current state research on genetics and its association with significant biological mechanisms. ...

Nebicapone (BIA 3-202; 1-[3,4-dihydroxy-5-nitrophenyl]-2-phenylethanone), a novel catechol-O-methyltransferase inhibitor, is mainly metabolized by glucuronidation. The purpose of this study was to characterize the major plasma metabolites of nebicapone following p.o. administration of nebicapone to healthy volunteers, and to determine the human UDP-glucuronosyltransferase (UGT) enzymes involved...

Accumulating evidence indicates that mutations in the human UGT1 gene locus abolish hepatic bilirubin UDP-glucuronosyltransferase activity and cause the subsequent accumulation of bilirubin to toxic levels in patients with Crigler-Najjar type 1 (CN-I). Genetic and biochemical criteria are required to link CN-I with mutations in UGT1. Here we present analysis of mutations at the UGT1 locus in th...

Denopamine is one of the oral beta(1)-adrenoceptor-selective partial agonists. Denopamine glucuronide is the most abundant metabolite in human, rat, and dog urine when administered orally. Species differences in denopamine glucuronidation were investigated with liver microsomes obtained from humans and experimental animals. In rat and rabbit, only the phenolic glucuronide was detected, whereas ...

The cDNA encoding a phenobarbital-inducible form of rat liver UDP-glucuronosyltransferase has been isolated, sequenced, and expressed to yield a catalytically active enzyme. The cDNA was found to be 1,961 nucleotides in length and to have an open reading frame of 1,590 nucleotides flanked by 25 and 346 base pairs of 5' and 3' untranslated regions, respectively. The open reading frame encodes a ...

Increased UDP-glucuronosyltransferase in rat hepatocyte nodules and hepatocellular carcinomas produced by feeding 2-acetylaminofluorene or N-nitrosomorpholine was studied using isozyme-selective substrates, antibodies, and DNA probes. UDP-glucuronosyltransferase (UDP-GT) activities toward 4-methylumbelliferone, 1-naphthol, and benzo[a]pyrene-3,6-quinol were reversibly increased by short term fe...

Glucuronidation is a critical and elimination process in the detoxification of many different exogenous and endogenous compounds (Radominska-Pandya et al., 1999; Tukey & Strassburg, 2001). Glucuronides account for ~35% of all phase II drug metabolites (Evans & Relling, 1999), including therapeutic drugs such as SN-38, which is the active antitumor metabolite of the prodrug irinotecan, as well a...