|
Conference Chairperson: John T. Hunt, Bristol-Myers Squibb, Princeton, NJ
Scientific Program Committee: Matthew A. Marx, Pfizer, San Diego, CA Brent R. Stockwell, Columbia University, New York, NY David A. Wink, National Cancer Institute, Bethesda, MD Cheryl L. Zimmerman, University of Minnesota College of Pharmacy, Minneapolis, MN
* - Short talk from proffered paper
| February 8 |
|
| 6:30-8:00 p.m. |
Keynote Lectures |
| |
Introduction of Dr. Larry J. Marnett John T. Hunt, Bristol-Myers Squibb, Princeton, NJ
Cyclooxygenase Inhibitors in Cancer Detection, Prevention, and Treatment Larry J. Marnett, Vanderbilt University, Nashville, TN
Introduction of Dr. Gregory L. Verdine Brent R. Stockwell, Columbia University, New York, NY
Interrogation, Recognition, and Repair of Damaged Bases in DNA Gregory L. Verdine, Harvard University, Cambridge, MA |
| 8:00 – 9:00 p.m. |
Welcome Dessert Reception |
|
|
| February 9 |
|
| 7:00 – 8:00 a.m. |
Continental Breakfast |
| 8:00 – 9:45 a.m. |
Session 1: Chemistry in Support of Cancer Target ID and Validation |
|
Session Chair: Brent R. Stockwell, Columbia University, New York, NY
Probing Cell Death with Small Molecules Brent R. Stockwell
Multi-dimensional Chemical Genetics in Cancer Alexis Borisy, CombinatoRx, Inc., Cambridge, MA
Title to be announced Benjamin F. Cravatt, Scripps, La Jolla, CA
*Disrupting the Rb-Raf-1 Protein-protein Interaction: A New Strategy for Anticancer Drug Design Nicholas J. Lawrence, Moffitt Cancer Center and Research Institute, Tampa, FL |
| 9:45-10:15 a.m. |
Coffee Break |
| 10:15 a.m.-12:00 p.m. |
Session 2: Chemistry in Support of Lead Discovery/Chemical Libraries |
|
Session Chair: Michael Foley, Broad Institute, Cambridge, MA
Natural Product-based Libraries for Chemical Biology and Drug Discovery Derek S. Tan, Memorial Sloan-Kettering Cancer Center
Build-couple-pair Strategy for Diversity-oriented Synthesis Yields Small Molecule that Binds Hedgehog and Blocks Its Signaling in Human Cells Michael Foley
Achieving Synthetic Control When Nature Abandon Selectivity Scott A. Snyder, Columbia University, New York, NY
* Establishment of Novel Antitumor Drugs Screening Method by Using Chemical Array Siro Simizu, RIKEN, Wako, Saitama, Japan |
| 12:00 – 1:30 p.m. |
Lunch on own or Professional Advancement Session |
| 1:30 – 3:15 p.m. |
Session 3: Chemistry in Support of Lead Discovery/Screening, Hit Validation, and Natural Products |
|
Session Chairperson: Steven E. Hall, Lync Pharma, Research Triangle Park, NC
Self-Selecting Drug Discovery: Nucleotide Affinity Resin-Based Screening for Simultaneous Hit and Target Identification Steven E. Hall
Beyond Natural Products: Function Oriented Synthesis and New Leads for Cancer and Overcoming Cancer Resistance Paul A. Wender, Stanford University, Stanford, CA
Concise Synthetic Analogs of FR901464: Anti-tumor Compounds Targeting the Spliceosome Thomas R. Webb, St. Jude Children's Research Hospital, Memphis, TN
* Carteriosulfonic Acids A-C: Inhibitors of GSK3-β Identified From a Wnt Signaling Assay Malcolm W. McCulloch, University of Utah, Salt Lake City, UT |
| 3:15 – 3:45 p.m. |
Coffee Break |
| 3:45 – 5:30 p.m. |
Session 4: Chemistry in Support of Lead Discovery/Chemoinformatics |
|
Session Chairperson: Patrick Zarrinkar, Ambit Biosciences, San Diego, CA
High Throughput Kinase Profiling: A New Approach to Lead Discovery Patrick Zarrinkar
A Systems Approach to Therapeutic Discovery John Westwick, Odyssey Thera, San Ramon, CA
In silico Discovery of Small Molecules Targeting Transcription Factors in Cancer and Inflammation Alan C. Rigby, Harvard Medical School, Boston, MA
*3D QSAR Analysis of Pyrazole Derivatives and the Design of Novel Benzimidazole Derivatives Leyte L. Winfield, Spelman College, Atlanta, GA |
| 5:30 – 7:30 p.m. |
Poster Session A and Cocktail Reception |
|
|
| February 10 |
|
| 7:00 – 8:00 a.m. |
Continental Breakfast |
| 8:00 – 9:45 a.m. |
Session 5: Chemistry in Support of Lead Optimization/Case Histories I |
|
Session Chair: Matthew A. Marx, Pfizer, San Diego, CA
The Discovery of BMS-641988: A Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer Aaron Balog, Bristol-Myers Squibb, Princeton, NJ
GDC-0449: A Small Molecule Antagonist of the Hedgehog Pathway James C. Marsters, Jr., Genentech, Inc., South San Francisco, CA
Discovery of Eltrombopag, a Small-Molecule, Oral Thrombopoietin Receptor Agonist: From Screening to the Clinic Juan I. Luengo, GlaxoSmithKline, Collegeville, PA
*Synthesis and Anti-Tumor Properties of Pyrazolopyrimidines: Potent, ATP Competitive, and Selective Inhibitors of the Mammalian Target of Rapamycin (mTOR) David J. Richard, Wyeth Discovery Medicinal Chemistry, Pearl River, NY |
| 9:45-10:15 a.m. |
Coffee Break |
| 10:15 a.m.-12:00 p.m. |
Session 6: Chemistry in Support of Cancer Drug Discovery/Case Histories II |
|
Session Chairperson: Danzhou Yang, University of Arizona, Tucson, AZ
DNA G-quadruplexes as Potential Anticancer Drug Targets Danzhou Yang
The Discovery and Development of Diaryl-acylsulfonamide (Tasisulam Sodium, ASAP): A Novel Class of Antitumor Agents for Solid Tumors Chuan Joe Shih, Eli Lilly Research Laboratories, Indianapolis, IN
From HTS to Clinic: Discovery of PF-4217903 as Potent and Exquisitely Selective c-Met Inhibitor Jean Cui, Pfizer Global R & D, San Diego, CA
* DNA Ligase Inhibitors Identified by Computer Aided Drug Design as Novel Cancer Therapeutics Xi Chen, University of Maryland, Baltimore, MD |
| 12:00 - 2:00 p.m. |
Poster Session B and Light Lunch |
| 2:00 – 3:45 p.m. |
Session 7: Chemistry in Support of Cancer Drug Targeting, Drug Delivery, and Drug Disposition I |
|
Session Chairperson: Frederick W. Goldberg, AstraZeneca, Inc., Macclesfield, United Kingdom
Antibody-Drug Conjugates for Cancer Therapy Peter D. Senter, Seattle Genetics, Inc., Bothel, WA
Chemical Modifications for Making Drugs out of RNA Interference Kallanthottathil G. Rajeev, Alnylam, Cambridge, MA
Use of Phosphate Prodrugs to Improve Solubility: Development of AZD1152, a Soluble and Selective Aurora B Kinase Inhibitor Frederick W. Goldberg
*New Chemical Probes for Site-Directed Targets Generated by Focused Ultrasound Daniel Lee, The Methodist Hospital Research Institute, Houston, TX |
| 3:45 – 4:15 p.m. |
Coffee Break |
| 4:15 – 6:00 pm. |
Session 8: Chemistry in Support of Cancer Drug Targeting, Drug Delivery, and Drug Disposition II |
|
Session Chairperson: Cheryl L. Zimmerman, University of Minnesota, Minneapolis, MN
Multifunctional Nanotherapeutics for Cancer Treatment Tamara Minko, Rutgers University, New Brunswick, NJ
Surface-functionalization of Nanoparticles for Multi-targeted Drug Delivery Jayanth Panyam, University of Minnesota, Minneapolis, MN
Folate Targeted Therapies for Cancer Christopher P. Leamon, Endocyte, West Lafayette, IN
*Protein-passivated Fe3O4 Nanoparticles: Low Toxicity and Rapid Heating for Thermal Therapy Haoheng Yan, University of Massachusetts, Amherst, MA |
|
|
| February 11 |
|
| 7:00 – 8:00 a.m. |
Continental Breakfast |
| 8:00 – 9:45 a.m. |
Session 9: Chemistry in Support of Cancer Drug Discovery and Development I |
|
Session Chairperson: David A. Wink, Jr., National Cancer Institute, Bethesda, MD
Molecular Imaging Studies in Cancer Murali Krishna, National Cancer Institute, Bethesda, MD
Role of Hyperpolarized 13C Spectroscopic Imaging in Drug Development John Kurhanewicz, University of California, San Francisco, San Francisco, CA
Measuring Spatial and Temporal Molecular Changes in Tissues Using Imaging Mass Spectrometry Richard M. Caprioli, Vanderbilt University, Nashville, TN
*Semi-Synthesis of a Hydrocarbon-Stabilized Transcription Factor, Max Eileen J. Kennedy, Harvard University, Cambridge, MA |
| 9:45 – 10:15 a.m. |
Coffee Break |
| 10:15 a.m. - 12:00 p.m. |
Session 10: Chemistry in Support of Cancer Drug Discovery and Development II |
|
Session Chairperson: John T. Hunt, Bristol-Myers Squibb, Princeton, NJ
ABT-869: Process Development on a VEGF Inhibitor for the Treatment of Cancer Albert Kruger, Abbott Laboratories, North Chicago, IL
Microheterogeneity and Analytical Approaches to Macromolecules Randal B. Bass, Amgen, Inc., Seattle, WA
Systems and Controls for Handling Potent Anticancer Agents Rebecca Ahn, Ash Stevens, Inc., Detroit, MI
*V-PROLI/NO: A Liver Selective Nitric Oxide Prodrug Sam Hong, National Cancer Institute, Frederick, MD |
| Departure |
|
|
| |