SUNDAY |
2:00 pm - 9:00 pm | Arrival and Check-in |
6:00 pm | Dinner |
7:30 pm - 7:35 pm | Welcome / Introductory Comments by GRC Site Staff |
7:35 pm - 9:30 pm | Disrupting Protein-Protein Interactions |
| Discussion Leader: Matthew Marx (Takeda) |
7:35 pm - 8:05 pm | Robert Borzilleri (BMS)
"The Discovery of Millamolecules for Inhibiting Protein-Protein Interactions" |
8:05 pm - 8:15 pm | Discussion |
8:15 pm - 8:45 pm | David Rees (Astex)
"Fragment-Based Discovery of Novel Inhibitors of IAPs" |
8:45 pm - 8:55 pm | Discussion |
8:55 pm - 9:25 pm | Lewis Pennington (Amgen)
"Disruptors of the GK-GKRP Binding Interaction for Diabetes" |
9:25 pm - 9:30 pm | Discussion |
9:30 pm - 11:00 pm | Poster Session / Social Hour |
| Discussion Leader: Brock Shireman (Janssen) |
MONDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Taking Aim at Cancer: On Target Approaches |
| Discussion Leader: Gregory Ott (Teva) |
9:00 am - 9:30 am | Alexander Mazin (Drexel University)
"Small Molecule Inhibitors of the Homologous Recombination Proteins" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Jon Roffey (Cancer Research Technology, CRUK)
"Targeting Deregulated Tumour Cell Polarity Through Inhibition of Atypical Protein Kinase C" |
10:10 am - 10:20 am | Discussion |
10:20 am - 10:50 am | Coffee Break |
10:50 am - 11:20 am | Ray Finlay (AstraZeneca)
"The Discovery of AZD9291: A Mutant Selective EGFR Inhibitor" |
11:20 am - 11:30 am | Discussion |
11:30 am - 12:00 pm | Christopher Brain (Novartis)
"The Discovery of LEE011, a Selective Inhibitor of CDK4/6" |
12:00 pm - 12:10 pm | Discussion |
12:10 pm - 12:30 pm | General Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time (Optional Organized Mt. Kearsarge Hike Available) |
4:00 pm - 6:00 pm | Poster Session / Social Hour |
| Discussion Leader: Brock Shireman (Janssen) |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Drug Discovery Driven by Chemistry |
| Discussion Leader: Takashi Tsukamoto (Johns Hopkins University) |
7:30 pm - 8:00 pm | Jonathan E. Wilson (Merck)
"Impact of Kit-Based Catalysis Screening Methodology on Drug Discovery at Merck" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Leonard Winneroski (Eli Lilly)
"Highly Regio- and Diastereoselective Syntheses of Conformationally Constrained Non-Peptidic Beta-Secretase Inhibitors" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Frank Fang (Eisai)
"Post-Eribulin Natural Product-Driven Drug Discovery Efforts" |
9:20 pm - 9:30 pm | Discussion |
9:30 pm - 11:00 pm | Poster Session / Social Hour |
| Discussion Leader: Brock Shireman (Janssen) |
TUESDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Advances in Neurodegeneration |
| Discussion Leader: Silvana Leit (Galenea) |
9:00 am - 9:30 am | Celia Dominguez (CHDI)
"Discovery and Development of Potential Therapeutics for Huntington's Disease" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Stephan Schilling (ProBiodrug, Germany)
"Discovery and Development of Glutaminyl Cyclase Inhibitors: A New Approach for the Treatment of AD" |
10:10 am - 10:20 am | Discussion |
10:20 am - 11:00 am | Group Photo / Coffee Break |
11:00 am - 11:30 am | Jeffrey Axten (GSK)
"The PERK Inhibitor GSK2606414 and Translational Control in Neurodegeneration - Breakthroughs and Opportunities" |
11:30 am - 11:40 am | Discussion |
11:40 am - 12:10 pm | Dario Doller (Lundbeck)
"From 'Flat SAR' to Super-PAMs: Allosteric Modulation at the mGlu4 Receptor" |
12:10 pm - 12:20 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time (Optional Soccer, Softball and Hiking Activities Available) |
4:00 pm - 6:00 pm | Poster Session / Social Hour |
| Discussion Leader: Brock Shireman (Janssen) |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Increasing the Chance of Clinical Success in Oncology |
| Discussion Leader: Silvina Garcia Rubio (Helsinn Therapeutics) |
7:30 pm - 8:00 pm | Olivier Michielin (Department of Oncology, Lausanne, Switzerland)
"Translational Medicine: From Theory to the Patient Bedside" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | John deGroot (MD Anderson Cancer Center)
"High Throughput Screening to Identify Effective Agents for the Treatment of Molecular Glioblastoma Subtypes" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Peter Dragovich (Genentech)
"Mechanism-Based Toxicities Associated with NAMPT Inhibition and Related Mitigation Strategies" |
9:20 pm - 9:30 pm | Discussion |
WEDNESDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Rare and Neglected Diseases |
| Discussion Leader: Robert Jacobs (Anacor) |
9:00 am - 9:30 am | Wes Van Voorhis (University of Washington)
"Calcium-Dependent Protein Kinases: Novel Target for Therapy of Cryptosporidiosis, Toxoplasmosis, Neosporosis, and for Stopping the Transmission of Malaria" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | David Barros (GSK)
"Novel Drug Candidates for the Treatment of Tuberculosis" |
10:10 am - 10:20 am | Discussion |
10:20 am - 10:50 am | Coffee Break |
10:50 am - 10:55 am | TBA (Poster Talk #1) |
10:55 am - 11:00 am | Discussion |
11:00 am - 11:05 am | TBA (Poster Talk #2) |
11:05 am - 11:10 am | Discussion |
11:10 am - 11:40 am | John McKew (TRND @ NIH)
"NCATS TRND Program: Lessons in Collaborative Therapeutic Development for Rare and Neglected Tropical Diseases" |
11:40 am - 11:50 am | Discussion |
11:50 am - 12:20 pm | Robert Marquis (GSK)
"RIP2 Kinase and Blau Syndrome" |
12:20 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time (Optional Vice Chair Elect Golf Scramble Available) |
4:00 pm - 6:00 pm | Poster Session / Social Hour |
| Discussion Leader: Brock Shireman (Janssen) |
6:00 pm | Dinner |
7:00 pm - 7:30 pm | Business Meeting |
| Nominations for the Next Vice Chair; Fill in Conference Evaluation Forms; Discuss Future Site and Scheduling Preferences; Election of the Next Vice Chair |
7:30 pm - 9:30 pm | Being Image-Conscious: PET Ligands in Drug Discovery |
| Discussion Leader: Joanne Bronson (BMS) |
7:30 pm - 8:00 pm | Robert Mach (University of Pennsylvania)
"The Role of PET in Drug Development and the Drug Validation Process" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Eric Hostetler (Merck)
"Design and Application of PET Tracers for Measuring In Vivo Target Engagement" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | David Donnelly (BMS)
"Design, Synthesis, and Development of Potent [11C] and [18F] Labeled LPA1R Antagonists for PET Imaging" |
9:20 pm - 9:30 pm | Discussion |
THURSDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Late-Breaking Topics |
| Discussion Leader: Christopher O'Donnell (Pfizer) |
9:00 am - 9:30 am | Jacob Schwarz (Genentech)
"Discovery of GDC-0994, a Potent and Selective ERK1/2 Inhibitor in Early Clinical Development" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Neil Johnson (GSK)
"The Discovery and Development of GSK2879552, a Mechanism Based Irreversible Inhibitor of the Histone Lysine Demethylase LSD1" |
10:10 am - 10:20 am | Discussion |
10:20 am - 10:55 am | Coffee Break |
10:55 am - 11:00 am | TBA (Poster Talk #3) |
11:00 am - 11:05 am | Discussion |
11:05 am - 11:35 am | Richard Mackman (Gilead)
"Discovery of Respiratory Syncytial Virus Fusion Inhibitor GS-5806 and Clinical Proof of Concept in a Human RSV Challenge Study" |
11:35 am - 11:45 am | Discussion |
11:45 am - 12:15 pm | Adam Hughes (Theravance)
"Discovery of TD-5959: A First-in-Class Dual Pharmacology Multivalent Muscarinic Antagonist and Beta-2 Agonist (MABA) for the Treatment of COPD" |
12:15 pm - 12:25 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time (Optional Bike Ride and Lake Sunapee Cruise Activities Available) |
4:00 pm - 6:00 pm | Poster Session / Social Hour |
| Discussion Leader: Brock Shireman (Janssen) |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Keynote Session |
| Discussion Leader: David Rotella (Montclair State University) |
7:30 pm - 8:30 pm | Peter Schultz (The Scripps Research Institute)
"A Chemist's Foray into Translational Research - From Stem Cells to the Genetic Code" |
8:30 pm - 9:00 pm | Discussion |
9:00 pm - 9:30 pm | General Discussion |
9:30 pm - 11:00 pm | Social Hour |
FRIDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am | Departure |