Conference Program
 
DRUG METABOLISM

July 10-15, 2005
Holderness School
Holderness, NH

Chair:
Larry C. Wienkers

Vice Chair:
Leslie Z. Benet

Welcome to the Drug Metabolism Gordon Research Conference page. The Drug Metabolism scientific program focuses on current frontiers of science concerning the metabolism and disposition of drugs and related xenobiotics. This conference has been a venue for outlining cutting-edge research in the field for nearly 35 years. We are excited about the program. A broad range of important topics including metabolism related cytochrome P450 oxidation reactions, metabolic based drug toxicities, enzyme expression and regulation, novel approaches in clinical development and analytical methodologies will be covered. Note that housing and meals are included in the registration fee. Participation in the poster sessions is encouraged. This year, we will request that those bringing a poster limit the poster size to 4 ft by 4 ft. Our Vice-Chair, Leslie Benet will be in charge of the poster session.

SUNDAY
2:00 pm - 9:00 pmArrival and Check-in
5:00 pm - 6:00 pmReception
6:00 pmDinner
7:30 pm - 9:30 pmKeynote Lecture
Paul R. Ortiz de Montellano, Ph.D. (University of California, San Francisco)
MONDAY
7:30 am - 8:30 amBreakfast
8:45 amGroup Photo
9:00 am - 12:30 pmAdvances in the Basic Knowledge of Cytochrome P450 Towards the Understanding of Drug Metabolism: Part 1 - Structure/Function
Discussion Leader: Stephen G. Sligar, Ph.D. (University of Illinois at Urbana-Champaign)
9:00 am - 9:45 am Michael R. Waterman, Ph.D. (Vanderbilt University)
"Streptomyces P450s are a Working Model for New Drug Design"
9:45 am - 10:30 amIlme Schlichting, Ph.D. (Max Planck Institute)
"Redoxactive Metal Complexes - Control of Activity via Molecular Architecture"
10:30 amCoffee Break
11:00 am - 11:45 amEric F. Johnson, Ph.D. (Scripps Research Institute)
"Recent Advances in Structural Characterization of Drug Metabolizing P450 Monooxygenases"
11:45 am - 12:30 pmRichard N. Armstrong, Ph.D. (Vanderbilt University)
"Kappa: A Different Glutathione Transferase Fold for Oxidative Metabolism and Catabolism"
12:30 pmLunch
1:30 pm - 5:00 pmFree Time
5:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:30 pm - 9:30 pmAdvances in the Basic Knowledge of Cytochrome P450 Towards the Understanding of Drug Metabolism: Part 2 - Oxidation Reactions
Discussion Leader: William M. Atkins, Ph.D. (University of Washington)
7:30 pm - 8:10 pm Jeffrey P. Jones, Ph.D. (Washington State University)
"Isotope Effects and the (Unified?) Mechanism of P450 Mediated Reactions"
8:10 pm - 8:50 pm Sason Shaik, Ph.D. (Hebrew University)
"Structure and Reactivity Patterns in P450 Enzymes"
8:50 pm - 9:30 pm Stephen G. Sligar, Ph.D. (University of Illinois at Urbana-Champaign)
"Intermediate States and Complexity of P450 Metabolism"
TUESDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmDrug Metabolism-Consequences to Toxicity / Pharmacology
Discussion Leader: Judy Bolton, Ph.D. (University of Illinois at Chicago)
9:00 am - 9:45 am Jim Fishbein, Ph.D. (University of Maryland)
"Molecular Aspects of Cancer Chemoprevention by Dithiolethiones"
9:45 am - 10:30 am Natalia Tretyakova, Ph.D. (University of Minnesota)
"Mass Spectrometry of DNA and Protein Lesions Induced by Bifunctional Electrophiles"
10:30 am Coffee Break
11:00 am - 11:45 amGregory R.J. Thatcher, Ph.D. (University of Illinois at Chicago)
"Nitric Oxide, Estrogens, and Oxidative Stress"
11:45 am - 12:30 pmJohn M. Essigmann, Ph.D. (Massachusetts Institute of Technology)
"Design of DNA Damaging Agents that Overcome the Apoptotic Blockade of Prostate Cancer Cells"
12:30 pmLunch
1:30 pm - 5:00 pmFree Time
5:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:30 pm - 9:30 pmExpression and Tissue Distribution of Drug Metabolizing Enzymes
Discussion Leader: Jeffery C. Stevens, Ph.D. (Pfizer)
7:30 pm - 8:10 pm J. Steven Leeder, PharmD, Ph.D. (The Children's Mercy Hospitals)
"Ontogeny and Tissue-Specific Expression of 'Drug' Metabolizing Enzymes Involved in Fetal Development"
8:10 pm - 8:50 pmXinxin Ding, Ph.D. (Wadsworth Center)
"Developmental Expression of Drug Metabolizing Enzymes in the Nasal Mucosa and Lung"
8:50 pm - 9:30 pm Ronald N. Hines, Ph.D. (Medical College of Wisconsin)
"Developmental Regulation of Human Hepatic FMO1 and FMO3: Molecular Mechanisms and Genetic Variability"
WEDNESDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmIntegrating Preclinical Information to Predict Human Drug Disposition
Discussion Leader: Timothy S. Tracy, Ph.D. (Univ. Minnesota)
9:00 am - 9:45 amLeslie Z. Benet, Ph.D. (Univ. of California-San Francisco)
"Predicting Drug Disposition via Application of a Biopharmaceutics Drug Disposition Classification System: Transport/Absorption/Elimination Interplay"
9:45 am - 10:30 amR. Scott Obach, Ph.D. (Pfizer)
"The Utilization of In Vitro Inhibition Data for Projecting Clinical Drug-Drug Interactions - Defining the Unknowns and Leveraging the Knowns"
10:30 am Coffee Break
11:00 am - 11:45 amMary Paine, Ph.D. (Univ. of North Carolina)
"Pre-Clinical and Clinical 'Appeels' Of Grapefruit Juice-Drug Interactions"
11:45 am - 12:30 pmTimothy S. Tracy, Ph.D. (Univ. of Minnesota)
"Enzyme (Mis)Behavior: The Effects of Atypical Kinetics and Genotype on Predictions of Drug Disposition and Drug-Drug Interactions"
12:30 pmLunch
1:30 pm - 5:00 pmFree Time
5:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:30 pm - 9:30 pmOral Presentations of Selected Posters
Discussion Leader: Henry W. Strobel, Ph.D. (University of Texas Medical School, Houston)
Viola Tamasi, Ph.D. (University of Louisville)
"Dehydroepiandrosterone increases PPARa transcriptional activity by increasing levels of non-phosphorylated receptor"
Melissa A Kramer (Medical College of Wisconsin)
"Identification of novel CYP2C9 promoter SNPs within the Hispanic population"
Justine L Lam (University of California, San Francisco)
"In Vitro and In Vivo Correlation of Hepatic Transporter Effects on Erythromycin (ERY) Metabolism"
Jed N Lampe (University of Washington)
"Probing the Cytochrome P450 3A4 Active Site with the Fluorescent Ligand TNS (2(p-Toluidino)naphthalene-6-sulfonate)"
Josh T Pearson (University of Washington)
"Surface Plasmon Resonance Analysis of Antifungal Azoles Binding to CYP3A4: Kinetic Resolution of Multiple Binding Orientations"
Dustin M Smith (University of Washington)
"Advancing the Human Serum Albumin-CYP2C9 Interaction; a Link Between Spectral and Kinetic Results"
THURSDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmInnovative Clinical Approaches in Underwriting Disposition Factors in Early Drug Development
Discussion Leader: Paul G. Pearson, Ph.D. (Amgen)
9:00 am - 9:45 amRichard Lalonde, Pharm D. (Pfizer)
"Pharmacokinetic / Pharmacodynamic Modeling to Facilitate Accelerated Drug Development"
9:45 am - 10:30 amScott Patterson, Ph.D. (Amgen)
"Biomarkers in Early Drug Development"
10:30 amCoffee Break
11:00 am - 11:45 amJenny Chien, Ph.D. (Eli Lilly & Co.)
"Integrating in vitro enzyme kinetics, pharmacokinetics and pharmacodynamics to yield predictive drug-drug interaction models to guide dosing strategy"
11:45 am - 12:30 pm Richard Hargreaves, Ph.D. (Merck & Co)
"PET Imaging Approaches in Drug Development"
12:30 pmLunch
1:30 pm - 5:00 pmFree Time
5:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:30 pm - 9:30 pmNovel Technology Approaches to Applied to Drug Discovery and Development Drug Metabolism
Discussion Leader: Kenneth R. Korzekwa, Ph.D. (Merck Research Laboratories)
7:30 pm - 8:10 pm Daniel E. Murnick, Ph.D. (Rutgers University)
"Laser Based Carbon-14 Atom Counting for Drug Metabolism Studies"
8:10 pm - 8:50 pmWilliam M. Atkins, Ph.D. (University of Washington)
"Cytochrome P450 and Ligand Dynamics Revealed by Optical Biosensors and Nanodiscs"
8:50 pm - 9:30 pm Thomas Rushmore, Ph.D. (Merck Research Laboratories)
"Advances in In Vitro Technologies for Drug Metabolism"
FRIDAY
7:30 am - 8:30 amBreakfast
9:00 amDepart
Last Updated: August 14, 2006