| SUNDAY |
| 2:00 pm - 9:00 pm | Arrival and Check-in |
| 5:00 pm - 6:00 pm | Reception |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | Keynote Lecture |
| |
| Richard Weinshilboum, M.D. (Dept of Pharmacology, Mayo Clinic/Mayo Graduate School of Medicine, Rochester, MN)
"Pharmacogenetics - Looking Forward" |
| MONDAY |
| 7:30 am - 8:30 am | Breakfast |
| 8:45 am | Group Photo |
| 9:00 am - 12:30 pm | Genetic and Biochemical Manipulation of In Vivo ADME Models |
| Discussion Leader: Christopher Kemper, Ph.D. (Taylor
Technology, Inc, Princeton, NJ) |
| David B. West, Ph.D. (Xenogen, Alameda, Ca)
"The Use of In Vivo Biophotonic Imaging for the Monitoring of Gene Expression in Transgenic Animals" |
| Bill Smith, Ph.D. (Pfizer, Groton, CT)
"Characterization of CNS Drugs in mdr1a/b Knockout Mice: Perspiration and Inspiration" |
| Keith Ward, Ph.D. (GlaxoSmithKline, King of Prussia, PA)
"The Use of Biochemical Inhibitors of Transporters and Metabolizing Enzymes in Drug Discovery" |
| Ronald Cannon, Ph.D. (NEIHS, Research Triangle Park, NC)
"Location, Location, Location: The Three Most Important Factors in a Ras Transgenic Model" |
| 12:30 pm | Lunch |
| 5:00 pm - 6:00 pm | Poster Session |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | The Role of Protein-Protein Interactions on Cytochrome P450 Function |
| Discussion Leader: Wayne Backes, Ph.D. (LSU Health Sciences Center, New Orleans, LA) |
| Anna L. Shen, Ph.D. (Dept of Oncology, University of Wisconsin, Madison, WI)
"NADPH-cytochrome P450 Reductase: Conformational Changes Relative to Catalysis and Substrate Binding" |
| Lucy Waskell, M.D., Ph.D. (Dept of Anesthesiology, University of Michigan, Ann Arbor, MI)
"Reduction of Oxyferrous Cytochrome P450 2B4 by Cytochrome P450 Reductase" |
| Wayne Backes, Ph.D. (LSU Health Sciences Center, New Orleans, LA)
"Direct Interactions Among Reductase and Multiple Cytochrome P450 Enzymes " |
| TUESDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am - 12:30 pm | In Vitro Approaches to Study Transport Proteins: What Can These Models Tell Us About In Vivo Drug Disposition? |
| Discussion Leader: Kim Brouwer, Ph.D. (University of North Carolina, Chapel Hill, NC) |
| Yuichi Sugiyama, Ph.D. (Tokyo, Japan)
"Integrated Use of Single and Double-Transfected MDCK Cells; Utility in Predicting Transporter-Mediated Drug Clearance and Drug Interactions In Vivo" |
| Catherine Booth-Genthe, Ph.D. (Merck and Co., West Point, PA)
"Utilization of the Vaccinia Virus-Bacteriophage T7 RNA Polymerase System to Identify Functionally Relevant Polymorphisms in Drug Transport Proteins" |
| Douglas Conklin, Ph.D. (Cancer Genome Centre, Cold Spring Harbor, NY)
"Theory and Application of RNAi in Mammalian Cells" |
| Kim Brouwer, Ph.D. (University of North Carolina, Chapel Hill, NC)
"Use of Sandwich-Cultured Hepatocytes to Predict Biliary Excretion of Drugs, Alterations in Hepatic Drug Transport and Mechanisms of Interaction" |
| 12:30 pm | Lunch |
| 5:00 pm - 6:00 pm | Poster Session |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | Realizing the Future of Drug Metabolism Through Mass Spectrometry |
| Discussion Leader: Kathleen Cox, Ph.D. (Schering Plough Research Institute, Kenilworth, NJ) |
| Walter Korfmacher, Ph.D., Kwokei Ng and Yungsheng Hsieh (Schering Plough Research Institute, Kenilworth, NJ)
"New Uses for Mass Spectrometry in a Drug Discovery Environment: Tissue Analysis and MS Imaging of Drugs" |
| Richard Armstrong, Ph.D. (Vanderbilt University, Nashville, TN)
"Protein Structure and Dynamics by Amide H/D Exchange Mass Spectrometry" |
| Kevin Bateman, Ph.D. (Merck Frosst Canada & Co., Montreal, Que)
"Analysis of Covalent Cytochrome P-450-Drug Adducts" |
| WEDNESDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am - 12:30 pm | Active Sites of P450s: From Models to Molecular Structures |
| Discussion Leader: Julian Peterson, Ph.D. |
| Pamela Williams, Ph.D. (Astex Technology Ltd, Cambridge, UK)
"Crystal Structure of a Human Cytochrome P450" |
| Michael Wester, Ph.D. (The Scripps Research Institute, La Jolla, Ca)
"Structures of Substrate Bound P450 2C5" |
| Emily Scott, Ph.D. (University of Texas, Medical Branch, Galveston, TX)
"Cytochrome P450 2B4 and Relevant Mutants" |
| Julian Peterson, Ph.D. (UT Southwestern Medical Centre, Dallas, TX)
"Fatty Acid Hydroxylation by P450BM-3: Rational Mutagenesis to Produce Important Molecules" |
| 12:30 pm | Lunch |
| 5:00 pm - 6:00 pm | Poster Session |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | Oral Presentations of Selected Posters |
| Discussion Leader: Henry Strobel, Ph.D. (Dept. Biochemistry and Molecular Biology, University of Texas Medical School, Houston) |
| Kyle E. Allen (University of Washington)
"Kinetics of Non-dissociative Sequential Metabolism of an 8-Alkyl Xanthine by Human P450 1A2" |
| Elizabeth M. Joshi (University of Virginia)
"Metabolic Studies of 2 Acetylbenzothiophene: Relevance to Zileuton Hepatotoxicity" |
| Donghak Kim (Vanderbilt University)
"Enzymatic Mechanism Analysis of 2-Amino-3,5-dimethylimidazo [4,5f] quinoline (MeIQ) N-Hydroxylation by Human P450 1A2 using Random Mutagenesis" |
| Winnie Y. Kim (University of California San Francisco)
"Changes in HIV Protease Inhibitor Pharmacokinetics and P-glycoprotein (P-gp/MDRI) Expression and Function by Sex-steroid Hormones during the Ovulatory Cycle" |
| Charles W. Locuson (Washington State University)
"A New Class of CYP 2C9 Inhibitors: Probing CYP 2C9 Specificity with High Affinity Benzbromarone Derivatives" |
| Yoshitane Nozaki (University of Tokyo)
"Analysis of Methotrexate Transport in Rat Kidney: Contribution of Organic Anion Transporters and Reduced Folate Carrier" |
| THURSDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am - 12:30 pm | Biotransformations: Pharmacological/Toxicological Effects |
| Discussion Leader: Larry Wienkers, Ph.D. (Pharmacia, Kalamazoo, WI) |
| Mark Grillo, Ph.D. (Pharmacia, Kalamazoo, WI)
"Reactive Intermediates of Acidic Drugs: Acyl-CoA Thioesters versus Acyl Glucuronides" |
| Judy Bolton, Ph.D. (University of Illinois, Chicago, IL)
"Role of quinones in equine estrogen carcinogenesis" |
| Timothy L. Macdonald, Ph.D. (University of Virginia, Charlottesville, VA)
"Chemical mechanisms of idiosyncratic drug reactions" |
| 12:30 pm | Lunch |
| 5:00 pm - 6:00 pm | Reception |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | Clinical Implications of Transporters |
| Discussion Leader: Richard Kim, M.D. (Vanderbilt University, Nashville, TN) |
| Grant R. Wilkinson, Ph.D., D.Sc., (Vanderbilt University, Nashville, TN)
"Modulation of MDR1 Transport to Increase Brain Drug Delivery" |
| David Bailey, Ph.D. (University of Western Ontario, London, Ont)
"Effect of Dietary Constituents on Intestinal Drug Transporters" |
| Bruno Hagenbuch, M.D. (University Hospital, Zurich, Switzerland)
"Inhibition of Transporters and Drug-Induced Hepatotoxicity" |
| FRIDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am | Depart |