SUNDAY |
2:00 pm - 9:00 pm | Arrival and Check-in (Office Closed 6:00 pm - 7:00 pm) |
5:00 pm - 6:00 pm | Welcome Mixer (Dining Center) |
6:00 pm | Dinner |
7:30 pm - 7:45 pm | Introductory Comments by GRC Site Staff / Welcome by Albert J. Robichaud, Conference Chair |
7:45 pm - 9:30 pm | Pathway and Phenotypic Screening in Target and Drug Discovery |
| Discussion Leader: Young Shin Cho (Novartis) |
7:45 pm - 8:10 pm | Sergey Kozmin (Univ of Chicago)
"Identification of the cellular target of leucascandrolide A and neopeltolide, Glycolysis inhbitors" |
8:10 pm - 8:20 pm | Discussion |
8:20 pm - 8:45 pm | Mike Foley (MIT)
"Small Molecule Microarray and Target ID Facilitate Probe Discovery" |
8:45 pm - 8:55 pm | Discussion |
8:55 pm - 9:20 pm | John Tallarico (Novartis)
"Chemistry-centric Discovery of New Targets" |
9:20 pm - 9:30 pm | Discussion |
9:45 pm - 10:45 pm | Poster Session / Social Hour |
| Discussion Leader: Janeta Popovici-Muller (Schering Plough) |
MONDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | New Prospects for the Treatment of Type 2 Diabetes |
| Discussion Leader: Scott J. Hecker (Metabasis Therapeutics) |
9:00 am - 9:30 am | Mark Erion (Metabasis Therapeutics)
"Design of Fructose 1,6-Bisphosphatase Inhibitors and Evaluation of their Safety, Tolerability and Glucose-Lowering Potential in Patients with Poorly-Controlled Type 2 Diabetes" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Ramakanth Sarabu (Roche)
"Glucokinase Activators - Discovery to POC" |
10:10 am - 10:20 am | Discussion |
10:20 am | Coffee Break / Group Photo |
11:00 am - 11:30 am | Rob Jones (Arena Pharma)
"Discovery of JNJ-28630355, a Potent & Selective Tri-substituted Pyrimidine GPR119 Agonist" |
11:30 am - 11:40 am | Discussion |
11:40 am - 12:10 pm | Bob Dow (Pfizer Global R&D)
"Discovery and Preclinical Pharmacology of PF-4620110: A Selective Inhibitor of DGAT-1 for the Treatment of Type-2 Diabetes" |
12:10 pm - 12:20 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 6:00 pm | Free Time (Organized Mt. Kearsarge Hike available) |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Antivirals |
| Discussion Leader: Manoj Desai (Gilead Sciences) |
7:30 pm - 8:00 pm | Paul M. Scola (Bristol-Myers Squibb)
"Inhibition of HCV" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | John McCauley (Merck)
"Discovery of MK-7009: A Novel Macrocyclic HCV NS3/4a Protease Inhibitor" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Mike Peel (Scynexis)
"Cyclophilin Inhibition: Targeting HCV Replication via Host-Protein Modulation" |
9:20 pm - 9:30 pm | Discussion |
9:45 pm - 10:45 pm | Poster Session / Social Hour |
| Discussion Leader: Janeta Popovici-Muller (Schering Plough) |
TUESDAY |
7:30 am - 8:30 am | Breakfast |
8:45 am - 9:00 am | Business Meeting (Part I) |
| (Nominations for Chair of the 2012 Meeting by Nominating Committee) |
9:00 am - 12:30 pm | Targeting the PI3K/AKT pathway for oncology: Recent advances in drug discovery |
| Discussion Leader: Jean-Cristophe Harmange (Constellation Pharma) |
9:00 am - 9:30 am | John Allen (Amgen)
"Azole-Based Inhibitors of AKT" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Kevin Freeman-Cook (Pfizer Global R&D)
"Discovery of a Selective Akt Inhibitor for the Treatment of Human Tumors" |
10:10 am - 10:20 am | Discussion |
10:20 am | Coffee Break |
11:00 am - 11:30 am | Mark Layton (Merck)
"MK-2206: Discovery of the First Oral Allosteric Akt Kinase Inhibitor" |
11:30 am - 11:40 am | Discussion |
11:40 am - 12:10 pm | Carlos Garcia-Echeverria (Novartis)
"Imidazo[4,5-c]quinoline derivatives - structure-based design and optimization of dual PI3K/mTOR inhibitors" |
12:10 pm - 12:20 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 5:00 pm | Free Time (Organized Annual East-West Softball Game) |
5:00 pm - 6:00 pm | Poster Session |
| Discussion Leader: Janeta Popovici-Muller (Schering Plough) |
6:00 pm | Dinner |
7:15 pm - 7:30 pm | Business Meeting (Part II) |
| (Speeches by the candidates for Chair of the 2012 meeting) |
7:30 pm - 9:30 pm | Sphingosine-1-phosphate signalling and immunomodulation |
| Discussion Leader: Zoran Rankovic (Schering-Plough) |
7:30 pm - 8:00 pm | Hugh Rosen (Scripps Institute)
"Chemical modulators of the S1P receptor system: the integrated biology underlying therapeutics" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Kevin Cusack (Abbott)
"S1P receptor agonist: MedChem hit to DC and pre-clinical PoC" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Nigel Cooke (Novartis)
"Discovery and optimisation of novel S1P-1 receptor modulators" |
9:20 pm - 9:25 pm | Discussion |
9:25 pm - 9:30 pm | Presentation of Poster Awards |
| Presenter: Janeta Popovici-Muller (Schering Plough) |
9:45 pm - 10:45 pm | Social Hour |
WEDNESDAY |
7:30 am - 8:30 am | Breakfast |
8:30 am - 9:00 am | Business Meeting (Part III) |
| (Election of Chair for the 2012 meeting; Discussion of 2012 meeting site; Fill out Conference Evaluation Forms) |
9:00 am - 12:30 pm | Preclinical Screening and Design Principles for Improved Drug Safety |
| Discussion Leader: Mark Noe (Pfizer Global R&D) |
9:00 am - 9:30 am | Tom Baillie (Univ of Washington)
"The Role of DMPK in Optimizing Drug Candidates for Safety" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | David Goldstein (Roche)
"Using In-Vitro Assays, including KinaseSelectivity Profiles, to Predict Toxicity In-Vivo" |
10:10 am - 10:20 am | Discussion |
10:20 am | Coffee Break |
10:55 am - 11:00 am | Poster Award 1: Oral Overview |
11:00 am - 11:30 am | Jim Empfield (Astra Zeneca)
"Physicochemical and pharmacological properties as predictors of drug safety and success" |
11:30 am - 11:40 am | Discussion |
11:40 am - 12:10 pm | Martin Edwards (Pfizer Global R&D)
"Drug Safety - Can we usefully separate structurally specific risks from physical property risks?" |
12:10 pm - 12:20 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 5:00 pm | Free Time (Organized Annual Vice-Chair Elect Golf Tournament) |
5:00 pm - 6:00 pm | Poster Session |
| Discussion Leader: Janeta Popovici-Muller (Schering Plough) |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | New Targets in Oncology |
| Discussion Leader: Matthew Marx (Pfizer Global R&D) |
7:30 pm - 7:35 pm | Poster Award 2: Oral Overview |
7:35 pm - 8:00 pm | Shawn Qian (Cytokinetics)
"CENP-E motor protein, Clinical candidate first disclosure, SAR and in vivo biology" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Mike Koehler (Genentech)
"The Discovery of the Hedgehog Antagonist GDC-0449 for the Treatment of Solid Tumors" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Ashvin Gavai (Bristol-Myers Squibb)
"Novel Androgen Receptor Antagonists: Lead Optimization & Preclinical Pharmacology" |
9:20 pm - 9:30 pm | Discussion |
9:45 pm - 10:45 pm | Social Hour |
THURSDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Late Breaking Topics |
| Discussion Leader: Sandra Filla (Eli Lilly) |
9:00 am - 9:30 am | Patrick Verhoest (Pfizer Global Research & Development)
"Identification of a PDE9 Clinical Candidate for the Treatment of Alzheimer's Disease Utilizing Prospective Design and Novel Protocol Development" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Lianhong Xu (Gilead)
"GS-9350: A Potent and Selective Pharmacoenhancer" |
10:10 am - 10:20 am | Discussion |
10:20 am | Coffee Break |
10:50 am - 10:55 am | Poster Award 3: Oral Overview |
10:55 am - 11:25 am | Philip A. Hipskind (Research Fellow, Lilly Research Laboratories)
"Novel CRH1 Antagonists for Anxiety Depression Alcohol Abuse" |
11:25 am - 11:35 am | Discussion |
11:35 am - 12:05 pm | Mark Bunnage (Pfizer Global Research & Development)
"Discovery of PF-610,355: An inhaled once-daily Beta-2 adrenoceptor agonist for treatment of asthma & COPD" |
12:05 pm - 12:15 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 5:00 pm | Free Time |
5:00 pm - 6:00 pm | Chair's Reception |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Chair's Speaker |
7:30 pm - 8:30 pm | Paul J. Reider (Princeton University) |
8:30 pm - 9:30 pm | General Discussion |
9:45 pm - 10:45 pm | Social Hour |
FRIDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am | Depart |