Conference Program
 
DRUG METABOLISM

July 8-13, 2001
Holderness School
Holderness, NH

Chair:
Cosette J. Serabjit-Singh

Vice Chair:
Jack P. Uetrecht

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

Last Updated: May 4, 2006