Strong inhibition of the human UDP-glucuronosyltransferase enzymes (UGTs) may lead to undesirable effects, including hyperbilirubinaemia and drug/herb-drug interactions. Currently, there is no good way examine inhibitory effects specificities compounds toward all important UGTs, side-by-side under identical conditions. Herein, we report a new, broad-spectrum substrate for UGTs its uses in scree...

A new human liver UDP-glucuronosyltransferase (HlugP4) has been cloned and expressed in cell culture. The expressed enzyme has a molecular mass of 56 kDa and preferentially catalysed the glucuronidation of halogenated and bulky alkyl phenols. The C-terminal half of the sequence (246 amino acids) is 96% identical with the same portion of HlugP1, whereas the N-terminal half of the deduced protein...

BACKGROUND AND OBJECTIVES Gilbert's syndrome is a chronic benign disease leading to recurrent jaundice and major unconjugated bilirubin increase that may be toxic after the use of routine medication. This report aimed at describing the anesthetic approach in Gilbert's syndrome patient submitted to videolaparoscopic surgery. CASE REPORT Female patient, 22 years old with Gilbert's syndrome, sub...

Since human colorectal tumors are insensitive to most chemotherapeutic agents, there is a need for the discovery of new drugs that would show activity against this disease. In an attempt to better appreciate the relevance of a widely used mouse colon tumor (colon adenocarcinoma Co38) as a screening model for human colorectal tumors, we compared the main phase I and phase II drug-metabolizing en...

BACKGROUND AND OBJECTIVE Crigler-Najjar syndromes type I and II and Gilbert's syndrome are familial unconjugated hyperbilirubinemias caused by genetic lesions involving a single complex locus encoding for bilirubin-UDP-glucuronosyltransferase which is involved in the detoxification of bilirubin by conjugation with glucuronic acid. Over the last few years a number of different mutations affectin...

In an attempt to better understand breast tumors sensitivity or resis tance to anticancer drugs, the main drug-metabolizing enzyme systems were evaluated in both breast tumors and their corresponding peritumoral tissues in 12 patients. The following enzymes were assayed by Western blot: cytochromes P-4SO (1A1/A2, 2B1/B2, 2C8-10, 2E1, 3A4); glutathione .S'-transferases (GST-a, -u, and -TI); and ...

244 words Introduction: 740 words Discussion: 2025 words Nonstandard Abbreviations: Abc, ATP-binding cassette; AhR, aryl hydrocarbon receptor; CAR, constitutive androstane receptor; Cyp, cytochrome P450; CV, conventional; DPGs, drug-processing genes; GF, germ-free; Gst, glutathione S-transferase; LC-MS/MS, liquid chromatography tandem mass spectroscopy; Papss, 3'-phosphoadenosine 5'phosphosulfa...

Jaundice associated with hypertrophic pyloric stenosis was recognised in three patients; previous reports have suggested that this is a possible early manifestation of Gilbert syndrome. Most patients with Gilbert syndrome are homozygous for a (TA)(7)TAA polymorphism in the gene promoter coding for bilirubin glucuronosyltransferase. Two of the reported patients were homozygous for the (TA)(7)TAA...