Sunday, July 8

Keynote - "Are Transporter Genes Responsible for Variation in Drug Response?"
Kathleen M. Giacomini, Ph.D., UCSF, San Francisco, CA

Monday July 9th, 2001

Regulation of Expression of Drug Metabolizing Enzymes

Discussion Leader: Patrick Maurel, INSERM U128, Montpellier France

1. Tissue specific expression of drug metabolizing enzymes: studies with UDP glucuronosyltransferases
   Peter Mackenzie, PhD, Flinders Medical Centre, Bedford Park SA , Australia
2. Role of the nuclear receptor PXR in xenobiotic and bile acid metabolism
   Steve Kliewer, Ph.D., GlaxoSmithKline, RTP, NC
3. Regulation of Xenobiotic Metabolism by SXR/PXR
   Ronald Evans, Salk Institute, San Diego, CA
4. Regulation of Drug Metabolism by CAR
   David Moore, Baylor College of Medicine, Houston, TX

Clinical Ramifications of Genetic Polymorphisms

Discussion Leader: Steven A. Wrighton, Lilly Research Laboratories, Indianapolis, IN

1. Genetically variable nicotine inactivation by CYP2A6: Role in smoking and novel treatment approaches.
   Rachel Tyndale, University of Toronto, Toronto, Canada
2. Clincial Pharmacogenetics of CYP2C19
   James Rae, PhD, Georgetown University Medical Center, Washington, DC
3. DNA Diversity in Genes Affecting CYP3A Activity
   Erin G. Schuetz, St. Jude Children's Research Hospital, Memphis, TN

Tuesday July 10th, 2001

Advances in Structural Studies of Drug Metabolizing enzymes

Discussion Leader: Julian A. Peterson, Ph.D., UT Southwestern Dallas, TX

1. P450 2C Active Site Topology
   Michael R. Wester, Ph.D., The Scripps Research Institute, La Jolla, CA
2. Sulfation Through the Looking Glass - Structural Insights into Sulfotransferase Function
   Michael Coughtrie, Ph.D., University of Dundee, Dundee, Scotland.
3. CYP51: A New Target of Opportunity for Structure Based Drug Design
   Michael R. Waterman, PhD, Vanderbilt University Sch. of Med., Nashville, TN
4. The Human Nuclear Xenobiotic Receptor PXR: Structural Determinants of Directed Promiscuity
   Matt Redinbo, Ph.D., University of North Carolina at Chapel Hill, NC

Functional Analysis/Models of Human Drug Disposition

Discussion Leader: Brian Burchell, University of Dundee, Dundee, Scotland

1. Functional Analysis of Two Human Cytosolic Sulfotransferases (SULT4A1 and SULT1A1)
   Rebecca B. Raftogianis, Ph.D., Fox Chase Cancer Center, Philadelphia, PA
2. GR-PXR/CAR/RXR cross-talk in human hepatocyte. A possible link between some physiopathological stimuli and drug metabolism capacity?
   Patrick Maurel, INSERM U128, Montpellier France
3. Pharmacoproteomics in drug development
   Frank Witzmann, IUPU Columbus, Columbus, IN

Wedesday July 11th, 2001

Computational Modelling of Drug Metabolism and transport

Discussion Leader: Theodore Liston, Pfizer, Groton, CT

1. Developing Mechanistic Models for Drug Metabolism
   Ken Korzekwa, Camitro Corporation, Menlo Park, CA
2. e-ADME: Predicting Bioavailability and Permeability
   Lawrence X. Yu, Food and Drug Adminstration, Rockville, MD
3. An In Silico Model of Trans-cellular Transport Assay for P-glycoprotein substrate Identification
   Vijay Gombar, Ph.D., GlaxoSmithKline, Research Triangle Park, NC

Selected Abstracts for Oral presentationt

Discussion Leader: Prof. Henry Strobel, University of Texas Medical School, Houston, TX

1. The Role of Water in P450BM-3
   Donovan C. Haines, Ph.D., University of Texas Southwestern Medical Center
2. Identifying the Importance of P-Glycoprotein and Cytochrome P450-3A4 in Intestinal Drug Metabolism: In Vitro Studies Using CYP3A4-Caco-2 Cells
   Carolyn L. Cummins, University of California San Francisco
3. Dapsone Activation of Multiple CP2C9 Substrates: Evidence for a Two-Site Binding Model
   James M. Hutzler, West Virginia University School of Pharmacy
4. Relative Reactivity of Radical Clock Probes for Detection of Aminium ion Intermediates in Enzymatic Oxidations
   Rheem A. Totah, University of Kansas
5. Photoaffinity labeling of P450 Cam using high specific activity 3H labeled benzophenone derivatives
   Michal J. Trnka, University of Washington
6. Genetic Variation in the Human Organic Cation Transporter hOCT2
   Maya Kaushal Leabman, University of California San Francisco

Thursday July 12th, 2001

Novel Approaches for Drug Discovery and Development

Discussion Leader: Lisa Shipley, Eli Lilly and Company, Indianapolis, IN

1. Profiling and Imaging of Peptides and Proteins in Biological Tissue sections by Mass Spectrometry
   Pierre Chaurand, PhD, Vanderbilt University, Nashville, TN
2. Using in vitro ADME profiles to select for in vivo evaluation in discovery
   Barbra Stewart, PhD, Ann Arbor Laboratories, Pfizer Global R & D
3. Automated assays for the extent and affinity of plasma protein binding: their application during drug discovery.
   Steve Wring, PhD, GlaxoSmithKline Inc., Research Triangle Park, NC

Biotransformation/Bioactivation

Discussion Leader: Jack Uetrecht, PhD, University of Toronto, Toronto, ON

1. Role of Drug Metabolism in Idiosyncratic Drug Toxicity: chemical, clinical and molecular perspectives
   Professor B Kevin Park, University of Liverpool, Liverpool
2. Evaluation of reactive metabolites in drug candidate selection
   Dr. Paul Pearson, Merck Research Laboratories, Rahway, NJ