Two human UDP-glucuronosyltransferases (UGTs), UGT2B7 and UGT1A1, catalyze the glucuronidation of many endo- and xenobiotics. Although UGT1A1 uniquely catalyzes the glucuronidation of the endobiotic, bilirubin, and UGT2B7 uniquely catalyzes the glucuronidation of morphine to both the 3-0 glucuronide and the 6-0 glucuronide, both catalyze the glucuronidation of the mixed opioid agonist/antagonis...

The human sulfotransferases (SULTs) regulate the activities of hundreds, if not thousands, of small molecule metabolites via transfer of the sulfuryl-moiety (-SO3) from the nucleotide donor, 3'-phosphoadenosine 5'-phosphosulfate (PAPS) to the hydroxyls and amines of the recipients. Our understanding of the molecular basis of SULT catalysis has expanded considerably in recent years. The basic ki...

Department of Biochemistry and Department of Human Genetics, Cardiovascular Research Laboratories, Cardiology Division, Faculty of Medicine, McGill University Health Centre/Royal Victoria Hospital, Montreal, Quebec, H3A 1A1, Canada. Department of Human Genetics, David Geffen School of Medicine at UCLA, Los Angeles, CA 90095, USA. Department of Medicine, Helsinki University Central Hospital, HUS...

1Department of Computer Science, National University of Singapore, 13 Computing Drive, Computing 2, #01-04, Singapore 117417 2UCL Interaction Centre, University College London, Gower Street, London WC1E 6BT, UK 3Knowledge Media Design Institute (KMDI), University of Toronto, 27 King’s College Circle, Toronto, Ont., Canada M5S 1A1 4Drexel University, 3141 Chestnut Street, Philadelphia, PA 19104,...

1. Department of Biochemistry, Hong Kong University of science & Technology, Clear Water Bay, Kowloon, Hong Kong, Peoples Republic of China. 2. School and Department of medicine, University of California, San Diego, La Jolla, CA 92095, USA. 3. Department of Oncology, University of Western Ontario, London, Ontario, Canada N6A, 4L6. 4. Molecular Oncology Group, Department of Medicine, McGill Univ...

Background and Objectives:Time-phasic development of nitrate tolerance in cardiovascular diseases is very important because it can contribute to the advent of blunted vasodilation or rebound ischemia even during continuous NTG treatment. In such a condition, we should change the therapeutic regimen of nitrate treatment to prevent the worsening of symptoms. Materials and Methods:We created a nit...

Methomyl (Lannate) is a pesticide widely used to control of insects in grape gardens. Methomyl treatment induces significant alteration in mixed function oxidase system. The present work was designed to study the inhibitory effect of methomyl on different forms of cytochrome P450 induced by phenobarbital (CYP 2B1, 2B2 and 3A) and benzo[a]pyrene induced (CYP 1A1). Adult male rats were divided in...

BACKGROUND Genetic polymorphisms of metabolizing enzymes may affect the risk of cancer formation in humans. Since the diet can contain polycyclic aromatic hydrocarbons (PAHs) and heterocyclic amines (HAs), the relationship between polymorphisms of enzymes involved in PAH and HA metabolism and the occurrence of sporadic colorectal cancer was studied. PATIENTS AND METHODS Five hundred colorecta...

Human UDP-glucuronosyltransferases (UGTs) play a pivotal role in phase II metabolism by catalyzing the glucuronidation of endobiotics and xenobiotics. The catalytic activities of UGTs are highly impacted by both genetic polymorphisms and oligomerization. The present study aimed to assess the inter-isoform hetero-dimerization of UGT1A1, 1A9, and 2B7, including the wild type (1A1*1, 1A9*1, and 2B...

Over 100 distinct disease-associated mutations have been identified in the breast-ovarian cancer susceptibility gene BRCA1. Loss of the wild-type allele in > 90% of tumors from patients with inherited BRCA1 mutations indicates tumor suppressive function. The low incidence of somatic mutations suggests that BRCA1 inactivation in sporadic tumors occurs by alternative mechanisms, such as interstit...