2021年4月8日 · In this study, to screen the inhibitors against hUGTs in a more efficient way, a new fluorescence-based microplate assay for high-throughput screening and evaluation of UGT inhibitors was constructed by devising and synthesizing a set of fluorogenic substrates for hUGTs.

2019年3月1日 · Recent advances in the development of UGT1A1 probes and their application for screening UGT1A1 inhibitors are summarized and discussed in this review for the first time. Furthermore, a long list of UGT1A1 inhibitors, including information on their inhibition potency, inhibition mode, and affinity, has been prepared and analyzed.

UGT Activity Assay / Ligand Screening Kit (Fluorometric) (ab273331) enables rapid measurement of native or recombinant UGT activity in biological samples such as liver microsomes and can also be used to assess the effect of drugs and other novel compounds on UGT activity.

2011年2月1日 · This study shows the utility of a luminogenic UGT assay in screening for potential UGT substrates and inhibitors, and for determining their IC 50 s and UGT specificity.

UGT酶利用葡萄糖醛酸为糖基供体，广泛催化内源性（如胆红素、脂肪酸、甾体类激素、食物中的化合物、药物、环境污染物等）和外源性化学物质发生结合反应，通常结合反应后的化合物更具水溶性，易于排出体外，从而起到解毒的作用。 但是这类结合反应存在一种 特殊情况，即 结合位点发生在羧基上，形成潜在的毒性代谢物 ── 酰基葡萄糖醛酸代谢产物，在代谢产物安全性评价（MIST）的指导原则中（扩展阅读： 一文读懂：FDA药物代谢产物安全性试验技术（MIST） …

Selective high-performance liquid chromatography-tandem mass spectrometry functional assays of authentic glucuronides for five major hepatic UGT probe substrates were developed: β-estradiol-3-glucuronide (UGT1A1), trifluoperazine-N-glucuronide (UGT1A4), 5-hydroxytryptophol-O-glucuronide (UGT1A6), propofol-O-glucuronide (UGT1A9), and zidovudine ...

We identified 29 inhibitors by monitoring raloxifene glucuronidation with recombinant UGTs. All of the inhibitors potently inhibited UGT1A1 activity, as well. We found that zafirlukast is a potent general inhibitor of UGT1As and a moderate inhibitor of UGT2Bs because it monitors 4-methylumbelliferone glucuronidation by recombinant UGTs.

We present a validated method for the simultaneous evaluation of drug-mediated inhibition of six major UGT isoforms, developed in human liver microsomes through the use of pooled specific UGT probe substrates (cocktail assay) and rapid liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis.

2012年2月22日 · Selective high-performance liquid chromatography-tandem mass spectrometry functional assays of authentic glucuronides for five major hepatic UGT probe substrates were developed:...

We also developed an effective UGT gene annotation tool, a fast structure prediction platform based on the optimized AlphaFold, and web tools for UGTs virtual screening and sugar donor prediction of unknown UGTs.