Sunday
2:00 pm - 9:00 pm
Arrival and Check-in
6:00 pm - 7:00 pm
Dinner
7:30 pm - 7:40 pm
Introductory Comments by GRC Site Staff / Welcome from the GRC Chair
7:40 pm - 9:30 pm
Novel Strategies Targeting Immunotherapies
Discussion Leader: Pamela Haile (GlaxoSmithKline, USA)
7:40 pm - 8:10 pm
David Harrison (NodThera, United Kingdom)
"The Identification and Development of Monocyte-Specific NLRP3 Inhibitors"
8:10 pm - 8:20 pm
Discussion
8:20 pm - 8:50 pm
Gail Seal (GlaxoSmithKline, United Kingdom)
"Design of a Myeloid-Targeted BET-Bromodomain Inhibitor"
8:50 pm - 8:55 pm
Discussion
8:55 pm - 9:25 pm
Scott Mlynarski (AstraZeneca, USA)
"Discovery of AZD0011, an Orally Bioavailable Arginase Inhibitor that Reactivates T-Cell Anti-Tumor Response"
9:25 pm - 9:30 pm
Discussion
Monday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Small Molecule Antivirals for the COVID-19 Pandemic and Beyond
Discussion Leaders: Izzat Raheem (Merck, USA) and Brad Savall (Plexium Inc., USA)
9:00 am - 9:30 am
Arnab Chatterjee (Calibr at Scripps Research, USA)
"Optimization of Oral and Inhaled Drug Combinations to Treat and Prevent CoV-2 Infections with Protease and Polymerase Inhibitors"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Dustin Siegel (Gilead, USA)
"New Remdesivir Formulations for Early Treatment of Respiratory Viral Infections"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Ramil Baiazitov (PTC Therapeutics, USA)
"Emvododstat (PTC299) Mechanism of Action Offers Versatility Across Therapeutic Areas, from AML to COVID-19"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Jamison Tuttle (Pfizer, USA)
"Design of a SARS-CoV-2 Main Protease Inhibitor Administered Orally for the Treatment of COVID-19"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
3:00 pm - 4:00 pm
The GRC Power Hourâ„¢
The GRC Power Hourâ„¢ is designed to address challenges women face in science and issues of diversity and inclusion. The program supports the professional growth of all members of our communities by providing an open forum for discussion and mentoring.
Organizers: H. Rachel Lagiakos (Schrödinger, USA) and Jennifer Riggs (Bristol Myers Squibb, USA)
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Rare and Tropical Disease Therapeutics
Discussion Leader: Darby Schmidt (Inzen Therapeutics, USA)
7:30 pm - 8:00 pm
Kaitlyn Logan (Merck, USA)
"Optimization of N-Heteroaryl Indazole LRRK2 Inhibitors for CNS Drug Discovery"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Sungtaek Lim (Sanofi, USA)
"Substrate Reduction Therapy with Thienopyridines for the Treatment of Metachromatic Leukodystrophy"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Brendan Crowley (Merck, USA)
"Next Generation Oxazolidinone Antibiotics for the Treatment of Tuberculosis"
9:20 pm - 9:30 pm
Discussion
Tuesday
7:30 am - 8:30 am
Breakfast
8:30 am - 9:00 am
Group Photo
9:00 am - 12:30 pm
Driving Drug Discovery with Synthetic Methods and Technologies
Designed by Danica Rankic (Pfizer, USA)
Discussion Leader: Matthew Volgraf (Genentech, Inc, USA)
9:00 am - 9:30 am
David Battersby (GlaxoSmithKline, United Kingdom)
"High-Throughput PROTAC Synthesis for Direct, Biological Assaying"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Christopher am Ende (Pfizer Inc., USA)
"Advancing Chemical Biology and Drug Discovery Through Innovative Chemistry"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Sophie Rousseaux (University of Toronto, Canada)
"Synthesis and Functionalization of Cyclopropanes and Cyclobutanes"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
David Thaisrivongs (Merck, USA)
"Synthetic Macrocyclic Peptides that Target Protein-Protein Interactions: The Discovery and Early Development of a PCSK9 Inhibitor"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Harnessing the Potential of Ubiquitin Ligases: Targets and Effectors for Protein Degradation
Discussion Leader: Jennifer Riggs (Bristol Myers Squibb, USA)
7:30 pm - 8:00 pm
Matthew Weiss (Kymera Therapeutics, USA)
"Discovery and Characterization of IRAKIMiDs: Degraders Targeting Both IRAK4 and IMiD Substrates for Oncology Indications"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Willem Nissink (AstraZeneca, United Kingdom)
"Orally Available ER-Targeting PROTACs with In Vivo Activity: Conception, Cascade, Construction and Conformational Understanding"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Frederick Cohen (Nurix Therapeutics, USA)
"Discovery and Evaluation of Small-Molecule Inhibitors of the E3 Ligase Casitas B-Lineage Lymphoma B (CBL-B)"
9:20 pm - 9:30 pm
Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Novel Pain and Addiction Therapeutics to Combat the Opioid Crisis
Discussion Leader: Lewis Pennington (Kymera Therapeutics, USA)
9:00 am - 9:30 am
Kurt Rasmussen (Delix Therapeutics, USA)
"NIDA's Efforts to Combat the Opioid Crisis"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Brian Aquila (Alkermes, USA)
"Design and Evaluation of Naltrexone Prodrugs as Long-Acting Injectables for Treating Addiction"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Nurulain Zaveri (Astraea Therapeutics, USA)
"Medicinal Chemistry Navigates the Crossroads for Nociceptin Opioid Receptor GPCR-Targeted Small-Molecules for Treating the Dual Opioid Crisis of Pain and Addiction"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Julia Haas (Pfizer Boulder R&D, USA)
"Discovery of Allosteric NTRK1 Inhibitors for the Treatment of Pain"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
How Cryo-EM Structures Are Enabling Drug Discovery
Discussion Leader: John Van Drie (Van Drie Research LLC, USA)
7:30 pm - 8:00 pm
Richard Henderson (MRC Laboratory of Molecular Biology, United Kingdom)
"Progress and Prospects for CryoEM in Structural Biology"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Seungil Han (Pfizer Inc., USA)
"Application of Cryo-EM for Structure-Based Design Against Membrane Protein Targets for Inflammation and Metabolic Disease"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
John Tellis (Genentech, USA)
"Structure-Based Design of a Novel Series of NaV1.7 Inhibitors Using Cryo-Electron Microscopy"
9:20 pm - 9:30 pm
Discussion
Thursday
7:30 am - 8:30 am
Breakfast
8:30 am - 9:00 am
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
9:00 am - 12:30 pm
Late-Breaking Topics: First Disclosures of Clinical Candidates
Discussion Leader: Erin DiMauro (Merck & Co., Inc., USA)
9:00 am - 9:30 am
Steven Van der Plas (iTeos Therapeutics, Belgium)
"Discovery of Inupadenant, a Novel A2A Receptor Antagonist that Retains Activity in Adenosine-Rich Microenvironments"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Antonio Romero (Cytokinetics, USA)
"The Discovery of CK-136, a Selective Cardiac Troponin Activator"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Dustin Mergott (Eli Lilly and Company, USA)
"Discovery and Early Clinical Development of LY3372689, an O-GlcNAcase (OGA) Enzyme Inhibitor"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
James Taylor (Gilead Sciences, USA)
"Discovery of GS-4875: A First in Class TPL2 Kinase Inhibitor for Inflammatory Diseases and Beyond"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Keynote Session: From Targeted Small Molecules to Targeted Cell Therapies
Discussion Leader: Cynthia Parrish (GlaxoSmithKline, USA)
7:30 pm - 8:30 pm
Julian Adams (Gamida Cell, USA)
"From Targeted Small Molecules to Targeted Cell Therapies"
8:30 pm - 8:55 pm
Discussion
8:55 pm - 9:15 pm
General Discussion
9:15 pm - 9:30 pm
Closing Remarks
Friday
7:30 am - 8:30 am
Breakfast
9:00 am
Departure