| SUNDAY |
| 2:00 pm - 9:00 pm | Arrival and check-in |
| 6:00 pm | Dinner |
| 7:30 pm - 7:45 pm | Welcome and Introduction
Jack Uetrecht, Chair
|
| 7:45 pm - 8:45 pm | Keynote Lecture |
| Fred P. Guengerich, Ph.D. (Director of the Center for Molecular Toxicology,
Vanderbilt University)
The History of Drug Metabolism: a Semipersonal View |
| MONDAY |
| 7:30 am - 8:30 am | Breakfast |
| 8:45 am | Photo |
| 9:00 am - 12:30 pm | DNA Microarrays: Analysis of Gene Expression in Drug Metabolism, Cancer Biology and Toxicology |
| Discussion Leader: Tom Rushmore, Ph.D. (Merck Research Laboratories, West Point, PA) |
| 9:00 am - 10:00 am | Tom Rushmore, Ph.D. (Merck Research Laboratories, West Point, PA)
"Application of DNA Microarrays in Drug Metabolism and Toxicity Studies" |
| 10:00 am | Coffee Break |
| 10:30 am - 11:30 am | Denis Grant, Ph.D. (Director of the Institute for Drug Research and Chairman of Pharmacology, University of Toronto)
"TBA" |
| 11:30 am - 12:30 pm | Khew-Voon Chin, Ph.D. (Dept. of Medicine and Pharmacology
Robert Wood Johnson Medical School)
"Pharmacogenomics: Anticancer Drug Resistance and Beyond" |
| 12:30 pm | Lunch |
| 1:30 pm - 5:00 pm | Free Time / View Posters |
| 5:00 pm - 6:00 pm | Poster Session with Authors |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | New Directions in Proteomics |
| Discussion Leader: Daniel Liebler, Ph.D. (College of Pharmacy, University of Arizona) |
| 7:30 pm - 8:30 pm | Daniel Liebler, Ph.D. (College of Pharmacy, University of Arizona)
"Mapping Protein Modifications with LC/MS and the SALSA Algorithm" |
| 8:30 pm - 9:30 pm | Gavin MacBeath, Ph.D. (Center for Genomics Research, Harvard University)
"Applications of Microarray Technology in Proteomics" |
| TUESDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am - 12:30 pm | Regulation and Function of Hepatic Transporters |
| Discussion Leader: Richard Kim, M.D. (Dept. of Clinical Pharmacology, Vanderbilt University) |
| 9:00 am - 10:00 am | Richard Kim, M.D. (Dept. of Clinical Pharmacology, Vanderbilt University)
"Drug Disposition: A Coordinated Interaction between Drug Transporters, CYPs and Nuclear Hormone Receptors" |
| 10:00 am | Coffee Break |
| 10:30 am - 11:30 am | John Schuetz, Ph.D. (Pharmaceutical Sciences, St. Judes Children's Research Hospital)
"Function and Regulation of the ABC Transporter, MRP4" |
| 11:30 am - 12:30 pm | Mary Vore, Ph.D. (Graduate Center for Toxicology, University of Kentucky)
"Regulation of Expression and Function of Mrp2" |
| 12:30 pm | Lunch |
| 1:30 pm - 5:00 pm | Free Time / View Posters |
| 5:00 pm - 6:00 pm | Poster Session with Authors |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | EVENING SESSION |
| Discussion Leader: Bob Hanzlik, Ph.D. (Dept. of Chemistry, University of Kansas) |
| 7:30 pm - 8:10 pm | Nico Vermeulen, Ph.D. / Jan Commandeur, Ph.D. (Dept. Pharmacology and Molecular Toxicology, Free University, Netherlands)
"Bioactivation and Bioinactivation of Selected Organoselenium Compounds" |
| 8:10 pm - 8:50 pm | Alfin Vaz, Ph.D. (Pfizer, Groton, CT)
"Mechanistic Studies on CYP-Catalyzed Oxidation of Terminal Olefins: Is the Oxometallacycle an Intermediate?" |
| 8:50 pm - 9:30 pm | Bob Hanzlik, Ph.D. (Dept. of Chemistry, University of Kansas)
"Cyclopropylamines as Probes of N-Dealkylation Mechanisms" |
| WEDNESDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am - 12:30 pm | Metabolite-Induced Adverse Drug Reactions |
| Discussion Leader: Mohammed Bourdi, Ph.D. (Dept. Molecular and Cell Toxicology, NIH)
|
| 9:00 am - 9:45 am | Narayan Avadhani, Ph.D. (University of Pennsylvania)
"Mechanisms of mitochondrial targeting of P450s and GSTs: Role in drug metabolism and toxicity" |
| 9:45 am | Coffee Break |
| 10:15 am - 11:00 am | Richard Aster, M.D. (Blood Research Institute and Medical College of Wisconsin)
"Immune-Mediated Blood Dyscrasias Induced by Drugs and Drug Metabolites" |
| 11:00 am - 11:45 am | Mohammed Bourdi, Ph.D. (Dept. Molecular and Cell Toxicology, NIH)
"Factors Regulating Immune Reactions Against Protein Adducts of Reactive Metabolites" |
| 11:45 am - 12:30 pm | Cynthia Ju, Ph.D. (Dept. Molecular and Cell Toxicology, NIH)
"Potential Role of the Liver in Preventing Immune Reactions Against Drug-Protein Adducts" |
| 12:30 pm | Lunch |
| 1:30 pm - 5:00 pm | Free Time / View Posters |
| 5:00 pm - 6:00 pm | Poster Session with Authors |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | Selected Abstracts for Oral Presentation |
| Discussion Leader: Henry Strobel, Ph.D. (Dept. Biochemistry and Molecular Biology, University of Texas Medical School, Houston) |
| 7:30 pm - 9:30 pm | Six 15 minute presentations to be announced |
| THURSDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am - 12:30 pm | Metabolism in Drug Discovery: Have We Really Made a Difference? |
| Discussion Leader: Deborah Nicoll-Griffith, Ph.D. (Dept. Medicinal Chemistry, Merck-Frosst Canada) |
| 9:00 am - 10:00 am | Kathleen Cox, Ph.D. (Schering Plough Research Institute, Kenilworth, NJ)
"Early metabolism characterization: 'Make or break' studies for discovery compounds" |
| 10:00 am | Coffee Break |
| 10:30 am - 11:30 am | Nathalie Chauret, Ph.D. (Merck Frosst Canada, Montreal, Canada)
"Early Intervention in Guiding Drug Candidate Structure" |
| 11:30 am - 12:30 pm | Jae Lee, Ph.D. (Pfizer, Groton, CT)
"Influencing Chemists to minimize attrition" |
| 12:30 pm | Lunch |
| 1:30 pm - 5:00 pm | Free Time / View Posters |
| 5:00 pm - 6:00 pm | Poster Session with Authors |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | Novel Biotransformation Pathways |
| Discussion Leader: Lewis Klunk, Ph.D. (Bristol-Myers Squibb, Princeton, NJ) |
| 7:30 pm - 7:50 pm | Wade Adams, Ph.D. (Pharmacia, Kalamazoo, MI)
"Biotransformation of a tetrahydro-4(2H)-thiopyranyl
phenyloxazolidinone sulfoxide" |
| 7:50 pm - 8:10 pm | Chandra Prakash, Ph.D. (Pfizer, Groton, CT)
"Unusual ring scission of nitrogen heterocycles" |
| 8:10 pm - 8:30 pm | Sanjeev Kumar, Ph.D. (Merck & Co)
"A novel CYP-catalyzed metabolism of diclofenac acyl glucuronide in human liver microsomes: potential impact on CYP2C9 activity phenotyping in humans in vivo" |
| 8:30 pm - 8:50 pm | Stephen Castellino, Ph.D. (Glaxo Smith Kline, Research Triangle Park, NC)
"Structures from the X-Files: The Story of GI262570 Metabolism" |
| 8:50 pm - 9:10 pm | Wei Tang, Ph.D. (Merck, Rahway, NJ)
"Isethionic acid conjugatation: Metabolism of a thiazole
benzenesulfonamide beta-3 adregenergic receptor agonist in rats" |
| 9:10 pm - 9:30 pm | Abdul Mutlib, Ph.D. (Pfizer, Ann Arbor, MI)
"Identification and characterization of unusual metabolites by LC/MS and LC/NMR" |
| FRIDAY |
| 7:30 am - 8:30 pm | Breakfast |
| 9:00 am | Departure |
