Symposia in the Drug Metabolism Area for the
XIVth World Congress of Pharmacology
July 7-12, 2002
San Francisco, CA
Role of Transporters in Drug Metabolism
Chair(s): Dr. Susan Cole and Dr. Richard Kim
Monday, July 8, 2:45 - 5:15
Uptake transporters and drug disposition
Richard B. Kim Vanderbilt University USA
P-Glycoprotein and drug bioavailability
Leslie Z. Benet UCSF School of Pharmacy USA
Biliary transporters and disease
R.J.P. Oude Elferink Academic Medical Center The Netherlands
Transport of xenobiotic metabolites by the MRP-related proteins
Susan Cole Queen's University Canada
In Vitro Models for the Prediction of Human Drug Metabolism and Clearance In Vivo
Chair(s): Dr. Donald Birkett and Dr. G.T. Tucker
Tuesday, July 9, 9:45 - 12:15
Introduction and overview of issues
Donald J. Birkett Flinders Medical Centre Australia
Quantitative in vitro/in vivo prediction: Incorporating population variability 6)
Summing up and the way forward
G.T. Tucker University of Sheffield UK
In vitro and in silico models for drugs eliminated by glucuronidation
J.O. Miners Flinders Medical Centre Australia
Interplay between drug transporters and metabolising enzymes
Yuichi Sugiyama University of Tokyo Japan
Pharmacophore modeling
Kenneth Korzekwa Camitro Corporation USA
Single Nucleotide Polymorphisms in Drug Metabolism
Chair(s): Dr. Erin Schuetz and Dr. Howard McLeod
Tuesday, July 9, 2:45 - 5:15
Genetic polymorphisms in the human cytochrome P450 2B6 gene and their relevance to phenotypic expression and function
Professor Ulrich W. Zanger Dr. Margarete Fischer-Bosch Inst of Clin Pharm Germany
Genetic factors underlying the variable expression of cytochrome P450 3A
Leszek Wojnowski Epidauros Beiotechnologie AG Germany
Moving towards genotyping for drug metabolising enzymes in patient care
Leif Bertilsson Huddinge University Hospital Sweden
Interethnic variability in genetic polymorphism
Howard McLeod Washington University School of Medicine USA
CYP3A5 or PXR sequence variations and phenotypic consequence
Erin Schuetz St. Jude Children's Research Hospital USA
Receptor-mediated cytochrome P450 induction
Chair(s): Dr. Gabrielle Hawksworth and Dr. Allan Okey
Wednesday, July 10, 9:45 - 12:15
Receptor-mediated P450 induction: Pharmacological and toxicological consequences
Gabrielle Hawksworth University of Aberdeen UK
Induction of CYP1A1, CYP1A2 and CYP1B1 via the AH receptor: Does genetic variation in the receptor matter in rodents or in humans?
Allan B. Okey University of Toronto Canada
Role of the phenobarbital response unit in the regulation of CYP2B gene expression by phenobarbital and other inducers
Alan Anderson Centre de Recherche de L'Hôtel-Dieu de Québec Canada
Regulation of xenobiotic metabolism by the nuclear receptor PXR
Steven Kliewer GlaxoSmithKline USA
Induction of CYP3A4, CYP2C8,9,19 and CYP2B6 in human hepatocytes: How does it
fit with modulation of CAR, PXR and RXR expression?
Patrick J.P. Maurel CNRS France
Structure-Function of Cytochromes P450: Implications for Drug Metabolism, Design & Therapy
Chair(s): Dr. James Halpert and Dr. Steven Wrighton
Thursday, July 11, 9:45 - 12:15
Bacterial model systems of mammalian cytochrome P450 metabolism
Paul R. Ortiz de Montellano UCSF USA
Structural studies of substrate interactions with microsomal cytochromes P450
Eric F. Johnson Scripps Research Institute USA
Molecular modeling of human cytochromes P450
David Lewis University of Surrey UK
Pharmacophore insights into the active sites of cytochromes P450
Sean Ekins Lilly Research Labs USA
Structural determinants of cytochrome P450 3A4 substrate specificity and
James R. Halpert University of Texas Medical Branch at Galveston USA
New Perspectives in Drug Conjugation
Chair(s): Dr. John Miners and Dr. Yasushi Yamazoe
Thursday, July 11, 2:45 - 5:15
Introductory comments - Drug conjugation enzymes: A 2002 perspective
John O. Miners Flinders Medical Center Australia
Drug conjugating enzymes: What we can learn from the Human Genome Project.
Yasushi Yamazoe Tohoku University Japan
UDP-Glucuronosyltransferase: A structural and molecular perspective
Peter I. Mackenzie Flinders University School of Medicine Australia
Characterisation of the structural basis for sulfotransferase activity
Michael W.H.Coughtrie University of Dundee UK
Arylamine N-acetyltransferase: Structure and SNPs
Edith Sim University of Oxford UK
Structure, function and mechanisms of glutathione S-transferase
Richard N. Armstrong Vanderbilt University USA
Biological Relevance of Cytochrome P450 Epoxygenase-Derived Eicosanoids
Chair (s): Dr. Darryl Zeldin and Dr. Deanna Kroetz
Thursday, July 11, 2:45 - 5:15
Overview of the cytochrome P450 arachidonic acid epoxygenase pathway and its biological relevance
Darryl C. Zeldin NIEHS, NIH USA
Epoxygenase-derived Eicosanoids and calcium signaling in endothelial cells
Wolfgang Graier University of Graz Austria
Epoxyeicosatrienoic acids endothelial-derived hyperpolarizing factors in the coronary circulation
Ingrid Fleming Klinikum der J. W. Goethe-Universitat Germany
Cytochrome P450 epoxygenase metabolites and the regulation of cerebral blood flow
David Harder Medical College of Wisconsin USA
Epoxyeicosatrienoic acids and the regulation of systemic blood pressure
Deanna Kroetz University of California at San Francisco USA
Summary and Future Directions
Darryl C. Zeldin NIEHS, NIH USA
Plenary Lectures
Magnus Ingelman-Sundberg (Karolinska Institute, Sweden)
Pharmacogenetics: An Opportunity for a safer and more efficient pharmacotherapy
Tuesday, July 9, 1:30 - 2:30
Urs Meyer (University of Basel, Switzerland)
Drug induction of cytochromes P450: The role of orphan nuclear receptors
Wednesday, July 10, 8:30 - 9:30
