| Tuesday, April 20 |
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3:00 - 7:30 PM
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Registration
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Macdonald Foyer
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6:30 - 7:30 PM
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Refreshments
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Macdonald Foyer
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7:30 - 8:30 PM
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Keynote Address (Joint)
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Macdonald ABCD
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Jeff Blaney,
Genentech, Inc.
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Stephen W. Fesik,
Vanderbilt University School of Medicine
Targeting Protein-Protein Interactions Using Fragment-Based Methods and Structure-Based Design
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8:30 - 8:45 PM
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Orientation for New Attendees and New Investigators
Keystone Symposia's Chief Scientific Officer, Dr. Andy Robertson, to lead discussion in a "What to Expect during your Attendance" for interested delegates.
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Macdonald ABCD
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| Wednesday, April 21 |
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7:00 - 8:00 AM
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Breakfast
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Frontenac
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8:00 - 11:00 AM
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New Opportunities in Small Molecule Drug Discovery (Joint)
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Macdonald ABCD
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Anna K. Mapp,
University of Michigan
Catching Transcriptional Activators in the Act
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James A. Wells,
University of California, San Francisco
Turning Enzymes on with Small Molecules
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Saul H. Rosenberg,
Abbott Laboratories
Antagonists of BCL-2 Family Proteins
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Raymond C. Stevens,
The Scripps Research Institute
Structure and Function of the G-Protein Coupled Receptor Family
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Atwood Cheung,
Novartis Institutes for BioMedical Research
Short Talk: A Chemical Proteomics Approach to Identify Tankyrase as a Novel, Druggable Cancer Target in the WNT Signaling Pathway
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9:20 - 9:40 AM
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Coffee Break
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Macdonald Foyer
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11:00 AM -
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On Own for Lunch and Recreation
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11:00 AM - 1:00 PM
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Poster Setup
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Frontenac
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1:00 - 10:00 PM
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Poster Viewing
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Frontenac
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4:30 - 5:00 PM
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Coffee Available
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Macdonald Foyer
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5:00 - 7:00 PM
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SBDD-Medchem Interface (Joint)
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Macdonald ABCD
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Jeff Blaney,
Genentech, Inc.
Unexpected Structure-Based Design Failures and Successes from Fragment Hits
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Arun K. Ghosh,
Purdue University
Structure-Based Design of Aspartic Acid Protease Inhibitors
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Andrew W. Stamford,
Schering-Plough Research Institute
Structure-Based Design of BACE Inhibitors
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Fabian Buller,
ETH Zurich
Short Talk: Small-Molecule Ligand Discovery by High-Throughput Sequencing
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7:00 - 8:00 PM
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Social Hour w/ Lite Bites
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Frontenac
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7:30 - 10:00 PM
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Poster Session 1
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Frontenac
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| Thursday, April 22 |
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7:00 - 8:00 AM
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Breakfast
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Frontenac
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8:00 - 11:00 AM
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Enabling Technologies for New Lead Discovery
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Macdonald CD
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George Hartman,
Novira Therapeutics
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Miles Congreve,
Heptares Therapeutics Ltd
Fragment and Biophysical Screening Approaches to GPCR Drug Discovery
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Thomas Franch,
Nuevolution A/S
Fragment Based Lead Discovery using Millions of Screening Compounds
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Thorsten Naumann,
Sanofi-Aventis Deutschland GmbH
Current and Future Aspects of Lead Finding for Kinase Inhibitors
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Gregg Siegal,
Leiden University
Short Talk: Into the Great Unknown: Fragment Based Drug Discovery on Membrane Proteins
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Erin E. Carlson,
Indiana University
Short Talk: Innovative Technologies for Natural Products Discovery
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9:20 - 9:40 AM
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Coffee Break
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Macdonald Foyer
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11:00 AM -
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On Own for Lunch and Recreation
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11:00 AM - 1:00 PM
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Poster Setup
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Frontenac
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1:00 - 10:00 PM
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Poster Viewing
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Frontenac
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4:30 - 5:00 PM
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Coffee Available
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Macdonald Foyer
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5:00 - 7:00 PM
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New Approaches for the Discovery of Protein Kinase Inhibitors
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Macdonald CD
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David H. Sherman,
University of Michigan
Novel Drug Leads from Natural Products and their Derivation from Microbial and Biosynthetic Diversity
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David G. Hangauer,
SUNY Buffalo
Discovery of KX2-391: A Phase II Src Signaling Inhibitor with a Second MOA
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Philip Sanderson,
Merck & Co., Inc.
The Discovery and Development of Allosteric Akt Inhibitors for the Treatment of Cancer
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7:00 - 8:00 PM
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Social Hour w/ Lite Bites
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Frontenac
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7:30 - 10:00 PM
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Poster Session 2
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Frontenac
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| Friday, April 23 |
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7:00 - 8:00 AM
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Breakfast
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Frontenac
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8:00 - 9:00 AM
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Special Lecture (Joint)
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Simon F. Campbell,
The Future of the Pharmaceutical Industry, A Personal Perspective
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9:00 - 9:30 AM
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Coffee Break
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Macdonald Foyer
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9:30 - 11:30 AM
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Discovery of New Drugs for Treatment of Hepatitis C
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Macdonald CD
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Makonen Belema,
Bristol-Myers Squibb
Hepatitis C Virus – An Overview of Progress Toward Effective Therapeutics
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John A. McCauley,
Merck Research Laboratories
HCV NS3/4a Protease Inhibitors
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Max Cummings,
Tibotec
Binding of the Macrocyclic Noncovalent Inhibitor TMC435 to its HCV NS3/NS4A Protease Target
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Makonen Belema,
Bristol-Myers Squibb
The Discovery of Potent HCV Inhibitors Targeting the NS5A Protein
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11:00 AM -
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On Own for Lunch and Recreation
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4:30 - 5:00 PM
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Coffee Available
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Macdonald Foyer
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5:00 - 7:00 PM
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Late-Breaking Stories of Application of Structure-Based Design to Discovery of Drug Candidates
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Macdonald CD
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William J. Greenlee,
Schering-Plough Research Institute
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Kimberly Anne Burkhard,
University of Maryland Baltimore
Short Talk: Identification of Small Molecules that Target ERK2 Docking Sites and are Selective Substrate Inhibitors
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Pooja Sharma,
Monash University
Short Talk: Structural Insights into Protein-Ligand Interactions of First Generation Small Molecule Inhibitors of Escherichia coli DsbA: An Application of Structure Assisted Fragment based Lead Generation
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Eric Martin,
Novartis
Short Talk: Protein Family-Based Molding with 2D Profile-Qsar and 3D Surrogate AutoShim Ensemble Docking
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Zhengrong Zhu,
GlaxoSmithKline
Short Talk: Confronting Reality: When Millions of Compounds are not Enough
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7:00 - 8:00 PM
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Social Hour w/ Lite Bites
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Frontenac
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| Saturday, April 24 |
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7:00 - 8:00 AM
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Breakfast
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Frontenac
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8:00 - 11:00 AM
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Candidate Attrition in the Pharmaceutical Industry (Joint)
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Macdonald ABCD
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Catherine E. Peishoff,
GlaxoSmithKline Pharmaceuticals
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Paul D. Leeson,
AstraZeneca R&D Charnwood
Overview: What Have We Learned about Attrition?
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Neil Weir,
UCB Pharma S.A.
Can Validated Targets for Biologicals Inform Small Molecule Discovery; Learning from both Approaches
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Martin Stahl,
F. Hofmann-La Roche Ltd
Small Molecule Conformational Preferences in Ligand Design
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William C. Pomerantz,
University of Michigan
Short Talk: Probing the Function and Mechanism of Small Molecule Artificial Transcriptional Regulators
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9:20 - 9:40 AM
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Coffee Break
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Macdonald Foyer
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11:00 AM -
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On Own for Lunch and Recreation
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4:30 - 5:00 PM
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Coffee Available
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Macdonald Foyer
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5:00 - 7:00 PM
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Small Molecules: Modeling and Properties (Joint)
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Macdonald ABCD
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William J. Greenlee,
Schering-Plough Research Institute
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Ruth M. Lightfoot-Dunn,
Amgen Inc.
Causes and Remedies for Candidate Attrition
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Marc K. Hellerstein,
University of California, Berkeley
Systems Biology: The Full Consequences of Hitting my Target
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Gregory L. Verdine,
Harvard University
Drugging Oncogenic Transcription Factors
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7:30 - 8:30 PM
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Social Hour w/ Lite Bites
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Frontenac
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8:00 - 11:00 PM
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Entertainment
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Frontenac
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| Sunday, April 25 |
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Departure
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