SUNDAY |
2:00 pm - 9:00 pm | Arrival and Check-in |
6:00 pm | Dinner |
7:15 pm - 7:30 pm | Welcome / Introductory Comments by GRC Site Staff |
7:30 pm - 9:30 pm | Phenotypic Screening |
| Discussion Leader: Bradley Tait (Proteostasis) |
7:30 pm - 8:00 pm | Michelle Palmer (Broad Institute)
"Integrating novel technologies to identify small molecules that drive translational research and therapeutics in cardiovascular disease" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | John Tellew (GNF)
"Discovery and optimization of purines for the ex vivo expansion of hematopoietic stem cells" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Sabine Hadida (Vertex)
"Discovery of VX-770 (Ivacaftor), a CFTR potentiator for the treatment of cystic fibrosis in G551D patients" |
9:20 pm - 9:30 pm | Discussion |
9:45 pm - 11:00 pm | Poster Session (Group A) / Social Hour |
| Discussion Leader: Cindy Parrish (GSK) |
MONDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Antibody Drug Conjugates |
| Discussion Leader: Christopher J. O'Donnell (Pfizer) |
9:00 am - 9:30 am | Peter Senter (Seattle Genetics)
"Potent antibody drug conjugates for cancer therapy: where we've been and where we're going" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Paul Polakis (Genentech)
"Arming antibodies for cancer therapy" |
10:10 am - 10:20 am | Discussion |
10:20 am - 10:50 am | Coffee Break |
10:50 am - 11:20 am | Matt Francis (University of California Berkeley)
"New site specific strategies for the chemical modification of proteins" |
11:20 am - 11:30 am | Discussion |
11:50 am - 12:20 pm | Pavel Strop (Rinat)
"Novel enzymatic site specific conjugation and the impact of conjugation site on stability and pharmacokinetics of antibody drug conjugates" |
12:20 pm - 12:30 pm | 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 |
| Discussion Leader: Cindy Parrish (GSK) |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Second Messenger Targets in Drug Discovery |
| Discussion Leader: James Barrow (Johns Hopkins) |
7:30 pm - 8:00 pm | Neil Press (Novartis)
"Solubility-driven optimization of PDE4 inhibitors, enabling an improved drug profile In humans" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Jian Jin (University of North Carolina)
"Discovery of biased ligands of dopamine D2 receptors" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Craig Lindsley (Vanderbilt University)
"Development of allosteric inhibitors of phospholipase D: engineering isoform selectivity and emerging therapeutic applications" |
9:20 pm - 9:30 pm | Discussion |
9:45 pm - 11:00 pm | Poster Session (Group B) / Social Hour |
| Discussion Leader: Cindy Parrish (GSK) |
TUESDAY |
7:30 am - 8:30 am | Breakfast |
8:45 am - 9:00 am | Business Meeting (Part I) |
| Nominations for Chair of the 2016 Meeting by the Nominating Committee |
9:00 am - 12:30 pm | Advances in High Throughput Screening |
| Discussion Leader: Michael D. Wendt (Abbvie) |
9:00 am - 9:30 am | Andrew Pope (GlaxoSmithKline)
"Discovery heuristics - improving the quality, success and economics of lead discovery via aggregated analyses" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Scott Galasinski (Abbvie)
"What did I miss? The strengths and weaknesses of screening assay selection" |
10:10 am - 10:20 am | Discussion |
10:20 am - 11:00 am | Group Photo / Coffee Break |
11:00 am - 11:30 am | John Mathias (Pfizer)
"Looking for novel modes & differentiated equity from Hit ID screening" |
11:30 am - 11:40 am | Discussion |
11:40 am - 12:10 pm | Adam Hill (Novartis)
"Drugging the 'undruggable': advances into novel target space" |
12:10 pm - 12:20 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 5:00 pm | Free Time (Optional soccer, softball and hiking activities available) |
5:00 pm - 6:00 pm | Poster Session (Group A) |
| Discussion Leader: Cindy Parrish (GSK) |
6:00 pm | Dinner |
7:15 pm - 7:30 pm | Business Meeting (Part II) |
| Candidate speeches; Announcement of poster awards |
7:30 pm - 9:30 pm | Neuropathic Pain |
| Discussion Leader: Carolyn Dzierba (Bristol-Myers Squibb) |
7:30 pm - 8:00 pm | Donna Hammond (University of Iowa)
"The elemental mechanisms and models of neuropathic pain" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Sarah Skerratt (Pfizer Neusentis)
"The discovery and optimization of a series of potent, selective and CNS restricted pan-Trk ligands" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Tom McCarthy (Spinifex Pharmaceuticals)
"The discovery and development of angiotensin type 2 (AT2) receptor antagonists to treat chronic pain" |
9:20 pm - 9:30 pm | Discussion |
9:45 pm - 11:00 pm | Poster Session / Social Hour |
WEDNESDAY |
7:30 am - 8:30 am | Breakfast |
8:30 am - 9:00 am | Business Meeting (Part III) |
| Election of Chair for 2016 Meeting |
9:00 am - 12:30 pm | Drug Delivery and Formulation: Pharmacological and Safety Benefits of Alternative Formulations and Routes of Administration |
| Discussion Leader: Laura C. Blumberg (Alkermes) |
9:00 am - 9:30 am | Anjali Kumar (Flexion Therapeutics)
"Pharmacokinetics, safety and efficacy of intra-articular FX005, a p38 MAP kinase inhibitor formulated in 50:50 poly(lactic-co-glycolic acid) microspheres" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Robert Clarke (Pulmatrix)
"A dense, highly dispersible novel dry powder platform (iSPERSE) for inhalation delivery of mono or combination therapeutics to the airway" |
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 / Discussion) |
10:55 am - 11:00 am | TBA (Poster Talk #2 / Discussion) |
11:00 am - 11:30 am | Tamara Minko (Rutgers University)
"Targeted drug delivery of chemotherapeutics utilizing nanoparticle and liposomal formulations" |
11:30 am - 11:40 am | Discussion |
11:40 am - 12:10 pm | Julius Remenar (Alkermes) |
12:10 pm - 12:20 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 5:00 pm | Free Time (Optional Vice-Chair-Elect Golf Scramble available) |
5:00 pm - 6:00 pm | Poster Session (Group B) / Social Hour |
| Discussion Leader: Cindy Parrish (GSK) |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | GPCR Structure and Function |
| Discussion Leader: Doris Riether (Boehringer-Ingelheim) |
7:30 pm - 8:00 pm | Christofer Tautermann (Boehringer-Ingelheim)
"The use of GPCR structures and homology models in lead optimization" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Robert Leurs (University of Amsterdam)
"Small is getting big in GPCR drug discovery" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Miles Congreve (Heptares)
"Identification of dual orexin and orexin-1 selective antagonists using structure based drug design" |
9:20 pm - 9:30 pm | Discussion |
9:30 pm - 11:00 pm | Poster Session / Social Hour |
| Discussion Leader: Cindy Parrish (GSK) |
THURSDAY |
7:30 am - 8:30 am | Breakfast |
8:30 am - 9:00 am | Business Meeting (Part IV) |
| Fill out Conference Evaluation Forms; Discuss future Site & Scheduling preferences |
9:00 am - 12:30 pm | Late-Breaking Topics |
| Discussion Leader: Simon Haydar (Eli Lilly) |
9:00 am - 9:30 am | James Sutton (Novartis)
"Medicinal chemistry, biology and pharmacology of selective inhibitors of CDK9: overcoming uncommon challenges between generations" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Sharan Bagal (Pfizer Neusentis)
"Discovery of selective Nav1.8 modulators for the treatment of chronic pain" |
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 / Discussion) |
11:00 am - 11:30 am | Brad Savall (Janssen)
"2-Aminopyrimidine histamine H4 antagonists; discovery to the clinic" |
11:30 am - 11:40 am | Discussion |
11:40 am - 12:10 pm | Chafiq Hamdouchi (Eli Lilly)
"Novel spiropiperidine acid derivatives as selective GPR40 agonists for the treatment of type 2 diabetes: distinguished PK properties and pharmacology" |
12:10 pm - 12:20 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time (Optional Lake Sunapee cruise and biking excursions available) |
4:00 pm - 6:00 pm | Poster Session |
| Discussion Leader: Cindy Parrish (GSK) |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Keynote Address |
| Discussion Leader: Mark Murcko (Disruptive Biomedical, LLC) |
7:30 pm - 8:30 pm | Jay Bradner (Harvard Medical School and Dana Farber Cancer Institute)
"Targeting Gene Regulation: The Next Frontier in Drug Discovery" |
8:30 pm - 9:30 pm | Discussion |
9:30 pm - 11:00 pm | Social Hour |
FRIDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am | Departure |