SUNDAY |
2:00 pm - 9:00 pm | Arrival and Check-in (Office Closed 6:00 pm - 7:00 pm) |
6:00 pm | Dinner |
7:30 pm - 7:40 pm | Introductory Comments by GRC Site Staff / Chair's Welcome by Roland Dolle (Cubist Pharmaceuticals) |
7:40 pm - 9:30 pm | Frontiers in Drug Discovery I |
| Discussion Leader: Craig Thomas (NIH/NHGRI) |
7:40 pm - 8:20 pm | Rishi Jain (Novartis)
"Chemical Biology: An Essential Tool for Pharma" |
8:20 pm - 8:35 pm | Discussion |
8:35 pm - 9:20 pm | P. Jeffery Conn (Vanderbilt University)
"Optimization and Functional Diversity of Allosteric Modulators of GPCRs" |
9:20 pm - 9:30 pm | Discussion |
MONDAY |
7:30 am - 8:30 am | Breakfast |
8:30 am | Group Photo |
9:00 am - 12:30 pm | Chemical Biology: Probes and Pathways |
| Discussion Leader: Joseph Salvino (Alliance Discovery) |
9:00 am - 9:25 am | Kate Carroll (Scripps - Florida)
"Painting the Cysteine Chapel: New Tools to Probe Oxidation Biology" |
9:25 am - 9:35 am | Discussion |
9:35 am - 9:55 am | Dirk Heerding (GlaxoSmithKline)
"Potent and Selective PDK1 Inhibitors Through Fragment Screening" |
9:55 am - 10:05 am | Discussion |
10:05 am - 10:30 am | Coffee Break |
10:30 am - 11:00 am | Jonathan Ellman (Yale University)
"A Substrate-Based Fragment Approach for Enzyme Inhibitor Discovery" |
11:00 am - 11:10 am | Discussion |
11:10 am - 11:40 am | Karl Gademann (University of Basel)
"Controlling Biological Processes by Synthetic Natural Products" |
11:40 am - 11:50 am | Discussion |
11:50 am - 12:20 pm | Nathanael Gray (Dana Farber Cancer Institute)
"Three Strategies for Overcoming Kinase Inhibitor Resistance in Bcr-Abl, EGFR, PDGFR and B-Raf" |
12:20 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session I |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Drug Discovery and Cheminformatics |
| Discussion Leader: Brian McGuinness (Venenum Biodesign) |
7:30 pm - 7:55 pm | Jason Lowe (Broad Institute)
"Diversity-Oriented Synthesis of a CNS-Focused Azetidine Library" |
7:55 pm - 8:00 pm | Discussion |
8:00 pm - 8:35 pm | Jake Wiener (J&J Pharmaceutical Research & Development)
"Intuitive Informatics Methods for Analyzing SAR in Complex Datasets: Application to a Cathepsin S Inhibitor Program" |
8:35 pm - 8:45 pm | Discussion |
8:45 pm - 9:20 pm | Bryan Roth (University of North Carolina, Chapel Hill)
"The Subterranean Pharmacology of Approved Medications" |
9:20 pm - 9:30 pm | Discussion |
TUESDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | High Throughput & Drug Discovery Technologies |
| Discussion Leader: Scott Wolkenberg (Merck) |
9:00 am - 9:25 am | Todd Graybill (GlaxoSmithKline)
"Hit Identification Using DNA-Encoded Libraries: A Case Study with Tachykinin Cell- Surface Receptor" |
9:25 am - 9:35 am | Discussion |
9:35 am - 10:00 am | David Nirschl (Bristol-Myers Squibb)
"Centralized Purification for Discovery Chemistry: Changing Drug Discovery One Compound at a Time" |
10:00 am - 10:10 am | Discussion |
10:10 am - 10:30 am | Coffee Break |
10:30 am - 11:00 am | Kevin Moeller (Washington University in St. Louis)
"Electrochemistry, Umpolung Reactions, and the Use of Microelectrode Arrays for Monitoring of Small Molecule-Receptor Interactions in 'Real-Time'" |
11:00 am - 11:10 am | Discussion |
11:10 am - 11:40 am | Scott Harrison (Merck)
"Identification of the beta-Amyloid Plaque PET Ligand [18F]MK-3328 via Parallel Synthesis" |
11:40 am - 11:50 am | Discussion |
11:50 am - 12:20 pm | Thomas McMurry (Anchor Therapeutics)
"Discovery of Biased GPCR Agonists Based on Intracellular Domains" |
12:20 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 6:00 pm | Free Time |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Synthetic Methodology and Chemical Neurobiology |
| Discussion Leader: Karin Worm (Avila Therapeutics) |
7:30 pm - 7:55 pm | Alan Rolfe (Kansas University) [2010 Poster Winner]
"Facilitated ROMP Protocols: From Mitsunobu to Flow" |
7:55 pm - 8:00 pm | Discussion |
8:00 pm - 8:35 pm | Tehshik Yoon (University of Wisconsin-Madison)
"Photocatalysis with Visible Light" |
8:35 pm - 8:45 pm | Discussion |
8:45 pm - 9:20 pm | Dirk Trauner (University of Munich)
"Optochemical Genetics" |
9:20 pm - 9:30 pm | Discussion |
WEDNESDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Drug Discovery and Enabling Synthetic Chemistry |
| Discussion Leader: Richard Hartley (University of Glasgow) |
9:00 am - 9:25 am | J. Robert Merritt (Kean University)
"A CCR1 Antagonist for Autoimmune Diseases: from Combichem Hit to Lead, to Clinical Candidate, to Academics" |
9:25 am - 9:35 am | Discussion |
9:35 am - 10:00 am | Jonathan Grob (Novartis)
"MIDA Boronates for Medicinal Chemistry: The Development of a Suite of Reactions Enabling Library Synthesis with MIDA Boronates" |
10:00 am - 10:10 am | Discussion |
10:10 am - 10:30 am | Coffee Break |
10:30 am - 10:55 am | Jin-Quan Yu (Scripps - San Diego)
"Diversity-Oriented Synthesis through Divergent C-H Functionalizations" |
10:55 am - 11:05 am | Discussion |
11:05 am - 11:35 am | Nick Terrett (Ensemble Therapeutics)
"Moving in New Circles: Exploiting Macrocycles for Drug Discovery" |
11:35 am - 11:45 am | Discussion |
11:45 am - 12:20 pm | Kevin Woller (Abbott)
"Reflections on 10 Years of HTOS at Abbott" |
12:20 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session II |
6:00 pm | Dinner |
7:00 pm - 7:30 pm | Business Meeting: Part I |
| Nominations for the next Vice Chair; Fill out Conference Evaluation Forms; Discuss future Site & Scheduling preferences |
7:30 pm - 9:30 pm | Synthetic Chemistry and Catalysis |
| Discussion Leader: Robert Goodnow (Hoffman-La Roche) |
7:30 pm - 7:55 pm | Olugbeminiyi Fadeyi (Vanderbilt University) [2010 Poster Winner]
"A General Approach to Medium Ring Azabicycles: Progress Towards the Total Syntheses of Stemaphylline, Grandisines A & D, Verticillatin C and Cremastrine" |
7:55 pm - 8:00 pm | Discussion |
8:00 pm - 8:35 pm | Corey Stephenson (Boston University)
"Photoredox Catalysis: Enabling Chemical Synthesis with Visible Light" |
8:35 pm - 8:45 pm | Discussion |
8:45 pm - 9:20 pm | Tobias Ritter (Harvard University)
"Late-Stage Fluorination for PET Imaging" |
9:20 pm - 9:30 pm | Discussion |
THURSDAY |
7:30 am - 8:30 am | Breakfast |
8:30 am - 9:00 am | Business Meeting: Part II |
| Vice Chair Nominee Talks; Election of the next Vice Chair |
9:00 am - 12:30 pm | Lead Finding for Oncology and Neurodegenerative Diseases |
| Discussion Leader: Sam Gerritz (Bristol-Myers Squibb) |
9:00 am - 9:45 am | Jeffery Kelly (Scripps - San Diego)
"Adapting Proteostasis to Ameliorate Loss- and Gain-of-Function Misfolding Diseases" |
9:45 am - 10:00 am | Discussion |
10:00 am - 10:20 am | Coffee Break |
10:20 am - 11:10 am | Paul Hergenrother (University of Illinois, Urbana Champaign)
"Elevated Protein Expression as a Target for Selective Anticancer Therapy" |
11:00 am - 11:10 am | Discussion |
11:10 am - 11:40 am | Stephen Condon (TetraLogic Pharmaceuticals)
"The Discovery and Development of Smac Mimetics for the Treatment of Cancer" |
11:40 am - 11:50 am | Discussion |
11:50 am - 12:20 pm | Brent Stockwell (Columbia University)
"Probing Cell Death with Small Molecules" |
12:20 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 6:00 pm | Free Time |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Frontiers in Drug Discovery II |
| Discussion Leader: Seung Bum Park (Seoul National University) |
7:30 pm - 8:20 pm | Alan Palkowitz (Lilly)
"Phenotypic Drug Discovery: A Globally Integrated Platform Approach for Innovation" |
8:20 pm - 8:35 pm | Discussion |
8:35 pm - 9:15 pm | Richard L. Elliott (Bill & Melinda Gates Foundation)
"Drug Discovery for Neglected Diseases: Challenges and Opportunities" |
9:15 pm - 9:30 pm | Discussion |
FRIDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am | Departure |