EC Number   |
Application |
Reference |
|---|
    2.4.1.17 | analysis |
after infection of Sf9 insect cells with increasing amounts of recombinant baculovirus, encoding either UGT1A9 or UGT2B7, the correlation between glucuronidation rates and degree of infection follows different trends, depending on whether activity is the actual activity measured or is corrected for UDP-glucuronosyltransferase expression level. Above a certain low level of infection, further increases in infection ratios lead to a large decline in normalized activity, presumably due to the presence of full-length but inactive enzyme in the sample. Inaccuracies in comparison of normalized activity between different batches of a recombinant UDP-glucuronosyltransferase can be reduced by lowering the degree of infection of the insect cells, in combination with careful monitoring of UDP-glucuronosyltransferase expression. Poly-His-containing peptides, fused to the UDP-glucuronosyltransferase C-terminus, allow sensitive immunodetection of expressed enzymes with monoclonal antibodies. A minor increase in the Km values has been detected in the His-tagged UDP-glucuronosyltransferases, but no changes in parameters such as the kinetic model and the effects of albumin addition |
719350 |
| 2.4.1.17 | diagnostics |
3-epideacetycinobufagin can be used specially to measure the catalytic activity of UGT2B7 in biological samples due to its exclusive substrate specificty for the compound |
737232 |
| 2.4.1.17 | diagnostics |
androgen glucuronidation by UGT2B17 is particularly interesting in doping control |
735649 |
| 2.4.1.17 | drug development |
drug development process aims to produce safe, effective drugs within a reasonable time and at a reasonable cost. Phase II metabolism (glucuronidation) can affect drug action and pharmacokinetics to a considerable extent. Extensive glucuronidation is an obstacle to oral bioavailability because the first-pass glucuronidation or premature clearance by UDP-glucuronosyltransferases of orally administered agents frequently results in poor oral bioavailability and lack of efficacy. Modeling of chemical entities/drugs for UGTs and their kinetic data can be useful in understanding the binding patterns to be used in the design of better molecules, analysis of first-pass glucuronidation by intestinal UGTs, including their topology, expression profile, and pharmacogenomics, and substrate selectivity at the binding pocket, structural requirements, and mechanism of enzyme actions, detailed overview |
736015 |
| 2.4.1.17 | medicine |
imidazoacridinone and triazoloacridinone drugs are glucuronidated in human liver |
719349 |
| 2.4.1.17 | medicine |
isoform UGT2A1 is an important detoxification enzyme in the metabolism of polycyclic aromatic hydrocarbons within target tissues for tobacco carcinogens, and functional polymorphisms in UGT2A1 may play a role in tobacco-related cancer risk |
720625 |
| 2.4.1.17 | medicine |
some drugs frequently coadministered with morphine (tamoxifen, tacrolimus, diclofenac, carbamazepine, imipramine, clomipramine, amitriptyline, diazepam, lorazepam and oxazepam) extensively inhibit the morphine 3- and 6-glucuronosyltransferase activities of UGT2B7. If patients receive morphine and these drugs simultaneously, the drug-drug interaction may change the levels of morphine and these glucuronides, resulting in altered analgesic efficacy and the risk of side effects |
673312 |
| 2.4.1.17 | medicine |
some male athletes have testosterone to epitestosterone values greater than the accepted threshold value 4.0, even without testosterone abuse. The main reason for such false-positive results in doping tests is a low epitestosterone glucuronide concentration but not a high level of testosterone glucuronide |
703416 |
| 2.4.1.17 | medicine |
the UGT1A6 splice variant isoform 2, detected in the liver and kidney, has no transferase activity for deferiprone. When UGT1A6_i2 is coexpressed with the classic UGT1A6_i1 isoform, velocity is reduced for deferiprone but remains similar for 4-nitrophenol or serotonin glucuronidation |
703415 |
| 2.4.1.17 | medicine |
UGT1A10 codon 139 polymorphism may be an important determinant in risk for tobacco-related cancers |
673300 |
