SUNDAY |
4:00 pm - 8:00 pm | Arrival and Check-in (Check-in Desk Closed 6:00 pm - 7:45 pm) |
6:00 pm | Dinner |
7:30 pm - 7:40 pm | Welcome / Introductory Comments by GRC Site Staff |
7:40 pm - 9:30 pm | Frontiers in Drug Discovery |
| Discussion Leader: Lisa Marcaurelle (Broad Institute) |
7:40 pm - 8:20 pm | James Wells (UCSF)
"Turning Enzymes ON with Small Molecules" |
8:20 pm - 8:35 pm | Discussion |
8:35 pm - 9:15 pm | Robert Gould (Epizyme)
"Epigenetics: The Present and Future of Cancer Therapeutics" |
9:15 pm - 9:30 pm | Discussion |
MONDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Hit to Lead / Medicinal Chemistry |
| Discussion Leader: Craig Lindsley (Vanderbilt University) |
9:00 am - 9:20 am | Samuel Gerritz (Bristol-Myers Squibb) "The Discovery and In Vitro Optimization of a Novel Class of PTPgamma Inhibitors" |
9:20 am - 9:30 am | Discussion |
9:30 am - 9:50 am | Scott Sutton (Pfizer) "Parallel Synthesis and Metabolite Indentification of Phenol Containing HSP90 Inhibitors" |
9:50 am - 10:00 am | Discussion |
10:00 am - 10:30 am | Coffee Break |
10:30 am - 11:00 am | Jurgen Dinges (Abbott) "Hit-to-Lead Efforts Towards Novel EP1 Inhibitors for Pain Modulation" |
11:00 am - 11:10 am | Discussion |
11:10 am - 11:40 am | Gebhard Thoma (Novartis) "Hit-to-Lead Chemistry on Chemokine Receptor Antagonists: Inhibitors of CXCR3 and CXCR4 in Transplantation" |
11:40 am - 11:50 am | Discussion |
11:50 am - 12:20 pm | Peter Hamley (Sanofi-Aventis) "Accelerated Drug Discovery through High Throughput Chemistry" |
12:20 pm - 12:30 pm | Discussion |
12:30 pm | Group Photo / Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 5:30 pm | Poster Session I |
5:30 pm - 7:30 pm | Chemical Biology |
| Discussion Leader: Angela Koehler (Broad Institute) |
5:30 pm - 6:20 pm | Clifton Barry (NIH) "High-Throughput Approaches to Understanding Vulnerabilities in the Metabolism of Mycobacterium Tuberculosis" |
6:20 pm - 6:30 pm | Discussion |
6:30 pm - 7:15 pm | Lisa Marcaurelle (Broad Institute) "Building a Unique Compound Collection through Diversity-Oriented Synthesis: It's All About Stereochemistry!" |
7:15 pm - 7:30 pm | Discussion |
8:00 pm | Dinner |
TUESDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | High Throughput Technologies |
| Discussion Leader: Samuel Gerritz (Bristol-Myers Squibb) |
9:00 am - 9:20 am | Wolfgang Klute (Pfizer)
"Learning More from Libraries: Monomer and Reaction Success" |
9:20 am - 9:30 am | Discussion |
9:30 am - 9:50 am | Kenneth Bair (Forma Therapeutics) "Adventures with CS Mapping" |
9:50 am - 10:00 am | Discussion |
10:00 am - 10:30 am | Coffee Break |
10:30 am - 11:00 am | Michael Naesby (Evolva Inc.) "Genetic Chemistry - A Synthetic Biology Platform for the Discovery of "Unnatural" Natural Compounds and their Directed Evolution" |
11:00 am - 11:10 am | Discussion |
11:10 am - 11:40 am | Angela Koehler (Broad Institute) "Tackling Challenging Targets with Small-Molecule Microarrays" |
11:40 am - 11:50 am | Discussion |
11:50 am - 12:20 pm | Daniel Varon Silva (Max Plank) "Automated Oligosaccharide Synthesis: A High Throughput Method for the Synthesis of GPI-Anchored Proteins and Glycoproteins" |
12:20 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 5:30 pm | Free Time |
5:30 pm - 7:30 pm | Chemical Biology |
| Discussion Leader: Paul Hanson (Kansas University) |
5:30 pm - 6:20 pm | Craig Lindsley (Vanderbilt University)
"Molecular Switches' on Allosteric Ligands that Modulate Modes of Pharmacology" |
6:20 pm - 6:30 pm | Discussion |
6:30 pm - 7:20 pm | Allen Annis (Aileron)
"High-Throughput Discovery and Characterization of Protein-Ligand Interactions by Affinity Selection-Mass Spectrometry" |
7:20 pm - 7:30 pm | Discussion |
8:00 pm | Dinner |
WEDNESDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Chemical Methodology and Library Development |
| Discussion Leader: Ann Rowley (Broad Institute) |
9:00 am - 9:20 am | Alexander Doemling (University of Pittsburg) "A Novel Approach to Small Molecule Protein-Protein Interaction Discovery: MDM2/4 p53" |
9:20 am - 9:30 am | Discussion |
9:30 am - 9:50 am | Rolf Breinbauer (Graz University of Technology) "The Tale of Two Enantiomers - Synthesis of Tool Compounds in Chemical Biology" |
9:50 am - 10:00 am | Discussion |
10:00 am - 10:30 am | Coffee Break |
10:30 am - 11:00 am | Paul Hanson (Kansas University) "Facilitated DOS Approaches to Sultam Libraries" |
11:00 am - 11:10 am | Discussion |
11:10 am - 11:40 am | Derek Tan (MSKCC) "Strategies and Tactics in the Synthesis of Natural Product-based Libraries" |
11:40 am - 11:50 am | Discussion |
11:50 am - 12:20 pm | Seung-Bum Park (Seoul National University) "Importance of Molecular Diversity using Privileged Substructures for Translational Science and Chemical Biology" |
12:20 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 5:30 pm | Poster Session II |
5:30 pm - 7:30 pm | Synthetic Chemistry / Catalysis |
| Discussion Leader: Martin Burke (University of Illinois) |
5:30 pm - 6:15 pm | Oliver Reiser (University of Regensburg) "Immobilized Catalysts towards Applications in High Throughput Chemistry and Flow Processes" |
6:15 pm - 6:30 pm | Discussion |
6:30 pm - 7:15 pm | Vy Dong (University of Toronto) "Mechanism-Inspired Strategies for Organic Synthesis" |
7:15 pm - 7:30 pm | Discussion |
7:30 pm - 8:00 pm | Business Meeting (Part I) |
| (Nominations for the next Vice Chair; Fill out Conference Evaluation Forms) |
8:00 pm | Dinner |
THURSDAY |
7:30 am - 8:30 am | Breakfast |
8:40 am - 9:00 am | Business Meeting (Part II) |
| (Next Vice Chair Candidates Statements; Election of the next Vice Chair) |
9:00 am - 12:30 pm | Medicinal and Synthetic Chemistry |
| Discussion Leader: Oliver Reiser (University of Regensburg) |
9:00 am - 9:20 am | Young-Tae Chang (National University of Singapore)
"LuminoGenomics by Diversity-Oriented Fluorescence Library Approach (DOFLA)" |
9:20 am - 9:30 am | Discussion |
9:30 am - 9:50 am | Andrew Phillips (University of Colorado) "Chemistry and Biology with Natural Products and Other Small Molecules" |
9:50 am - 10:00 am | Discussion |
10:00 am - 10:30 am | Coffee Break |
10:30 am - 11:00 am | James Barrow (Merck) "Neuroscience Drug Discovery" |
11:00 am - 11:10 am | Discussion |
11:10 am - 11:40 am | Alex Godfrey (Lilly) "The Virtual MedChem Lab - Making it Rea!" |
11:40 am - 11:50 am | Discussion |
11:50 am - 12:20 pm | Martin Burke (University of Illinois) "The Prospect of Molecular Prosthetics: Small Molecules with Protein-Like Functions" |
12:20 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 5:30 pm | Free Time |
5:30 pm - 7:30 pm | Frontiers in Drug Discovery |
| Discussion Leader: Robert Gould (Broad Institute) |
5:30 pm - 6:05 pm | Chris Abell (University of Cambridge) "Fragment-Based Approaches in Drug Discovery and Chemical Biology" |
6:05 pm - 6:15 pm | Discussion |
6:15 pm - 6:35 pm | Fred Berst (Novartis) "Hinge-less Inhibitors of Kinases" |
6:35 pm - 6:45 pm | Discussion |
6:45 pm - 7:20 pm | Alan Palkowitz (Lilly) "Phenotypic Drug Discovery: A Globally Integrated Platform Approach for Innovation" |
7:20 pm - 7:30 pm | Discussion |
7:30 pm - 8:00 pm | Business Meeting (Part III) |
| (Announce next Vice Chair; Discuss future Site & Scheduling preferences) |
8:00 pm | Dinner |
FRIDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am | Depart |