Sunday |
2:00 pm - 9:00 pm | Arrival and Check-in |
6:00 pm | Dinner |
7:30 pm - 7:40 pm | Welcome / Introductory Comments by GRC Site Staff |
7:40 pm - 9:30 pm | Frontiers in Chemical Biology |
| Discussion Leader: Lyn Jones (Pfizer, USA) |
7:40 pm - 8:10 pm | Craig Thomas (National Institutes of Health, USA) "Chemical Genetics: Letting Mechanism Lead the Way" |
8:10 pm - 8:15 pm | Discussion |
8:15 pm - 8:45 pm | Matthew Bogyo (Stanford University School of Medicine, USA) "Small Molecule Protease Probes as Optical Contrast Imaging Agents" |
8:45 pm - 8:50 pm | Discussion |
8:50 pm - 9:25 pm | Jeffrey Bode (ETH Zurich, Switzerland) "Synthetic Fermentation of Bioactive, Non-Ribosomal Peptides" |
9:25 pm - 9:30 pm | Discussion |
Monday |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Integrated Chemical-Biological Approaches / New Directions in Synthesis |
| Discussion Leader: Yimon Aye (Cornell University, USA) |
9:00 am - 9:30 am | Seung Bum Park (Seoul National University, South Korea) "FITGE-Based Target Identification for the Connection of Rational Drug Discovery with Phenotypic Screening" |
9:30 am - 9:35 am | Discussion |
9:35 am - 10:05 am | Deborah Hung (Broad Institute / Massachusetts General Hospital, USA) "Chemical Biological Approach to Reveal Novel Mechanisms Involved in Immune Response to Infection" |
10:05 am - 10:10 am | Discussion |
10:10 am - 10:40 am | Stephan Sieber (Technical University Munich, Germany) "Chemical Tools to Manipulate Bacterial Pathogenesis" |
10:40 am - 10:45 am | Discussion |
10:45 am - 11:15 am | Coffee Break |
11:15 am - 11:45 am | Matthew Clark (X-Chem, Inc., USA) "DNA-Encoded Library Technology: Overview, Lead Discovery, and Technology Development" |
11:45 am - 11:50 am | Discussion |
11:50 am - 12:25 pm | Timothy Cernak (Merck, USA) "A Common Platform to Enable Nanoscale Synthesis" |
12:25 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 |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Mechanisms and Molecules for Epigenetic Regulation |
| Discussion Leader: Qiu Wang (Duke University, USA) |
7:30 pm - 8:05 pm | William Pomerantz (University of Minnesota, USA) "Choosing the Right Halogen, Fluorinated Bromodomains for Small Molecule Discovery" |
8:05 pm - 8:10 pm | Discussion |
8:10 pm - 8:45 pm | Timo Stellfeld (Bayer Healthcare, Germany) "Discovery and Optimization of a Novel SMYD2 Chemical Probe" |
8:45 pm - 8:50 pm | Discussion |
8:50 pm - 9:25 pm | Danica Fujimori (University of California, San Francisco, USA) "Chromatin- and Small Molecule-Mediated Regulation of Histone Demethylases" |
9:25 pm - 9:30 pm | Discussion |
Tuesday |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Assessing Cellular Effects of Chemical Stimuli
/ New Approaches and Applications of Library Design |
| Discussion Leaders: Cornella-Taracido Ivan (Merck, USA) and Justin Rettenmaier (University of California, San Francisco, USA) |
9:00 am - 9:25 am | Steffen Renner (Novartis, Switzerland) "Gene Signature-Based Phenotypic High-Throughput Screens - Hit Calling and Beyond" |
9:25 am - 9:30 am | Discussion |
9:30 am - 9:55 am | Hanna Axelsson (Karolinska Institutet, Sweden) "Screening of Thymidylate Synthase Using the Cellular Thermal Shift Assay (CETSA) – A High Throughput Target Engagement Assay" |
9:55 am - 10:00 am | Discussion |
10:00 am - 10:25 am | Frederick Goldberg (AstraZeneca, United Kingdom) "Design of Novel Building Blocks to Enhance Drug Discovery" |
10:25 am - 10:30 am | Discussion |
10:30 am - 11:00 am | Group Photo / Coffee Break |
11:00 am - 11:25 am | Douglas Beshore (Merck and Co., Inc., USA) "Non-Catalytic Site Integrase Inhibitors: Parallel Chemistry and Computational Techniques Applied to Virtual Screening Hit Evolution" |
11:25 am - 11:30 am | Discussion |
11:30 am - 11:55 am | Cullen Cavallaro (Bristol-Myers Squibb, USA) "Fragment-Based Discovery of KAT II Inhibitors Using a High Throughput Chemistry Approach" |
11:55 am - 12:00 pm | Discussion |
12:00 pm - 12:25 pm | Jeremy Jenkins (Novartis Institutes for Biomedical Research, USA) "Machine Learning and Crowdsourcing for Smaller, Smarter Libraries" |
12:25 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 |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Chemistry and Biology of Natural Products |
| Discussion Leader: Jiyong Hong (Duke University, USA) |
7:30 pm - 8:05 pm | Seth Herzon (Yale University, USA) "Synthesis and Study of Complex Natural Products" |
8:05 pm - 8:10 pm | Discussion |
8:10 pm - 8:45 pm | Michael Fischbach (University of California, San Francisco, USA) "Insights from a Global View of Secondary Metabolism: Small Molecules from the Human Microbiota" |
8:45 pm - 8:50 pm | Discussion |
8:50 pm - 9:25 pm | Erick Carreira (ETH Zurich, Switzerland) "Biology and Chemistry of Human Derived Natural Products" |
9:25 pm - 9:30 pm | Discussion |
Wednesday |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Chemical Probes for Profiling and Perturbation / Selectivity and Dynamics |
| Discussion Leaders: Elizabeth Parkinson (University of Illinois at Urbana-Champaign, USA) and Russell Petter (Celgene, USA) |
9:00 am - 9:30 am | Hua Xu (Pfizer, USA) "Rational Targeting of Active Site Tyrosine Residues Using Sulfonyl Fluoride Probes" |
9:30 am - 9:35 am | Discussion |
9:35 am - 10:05 am | Eranthie Weerapana (Boston College, USA) "Chemical-Proteomic Strategies to Investigate Reactive Cysteines" |
10:05 am - 10:10 am | Discussion |
10:10 am - 10:40 am | Coffee Break |
10:40 am - 11:10 am | Ralph Mazitschek (Massachusetts General Hospital / Harvard Medical School, USA) "Chemogenomic Approaches to Spatiotemporal Regulation of HDAC Activity" |
11:10 am - 11:15 am | Discussion |
11:15 am - 11:45 am | Timothy Cardozo (New York University, USA) "Historeceptomics Signatures of Drug Action" |
11:45 am - 11:50 am | Discussion |
11:50 am - 12:25 pm | J. Michael Bradshaw (Principia Biopharma, USA) "Tailoring Residence Time Utilizing Reversible Covalent Cysteine Targeting" |
12:25 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 |
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 | Frontiers in Synthetic Chemistry |
| Discussion Leader: Milana Maletic (Merck, USA) |
7:30 pm - 8:05 pm | Neal Devaraj (University of Calfornia, San Diego, USA) "Advancing Tetrazine Ligations for Applications in Biotechnology" |
8:05 pm - 8:10 pm | Discussion |
8:10 pm - 8:45 pm | Olafs Daugulis (University of Houston, USA) "New Methods for Carbon-Hydrogen Bond Functionalization" |
8:45 pm - 8:50 pm | Discussion |
8:50 pm - 9:25 pm | Phil Baran (The Scripps Research Institute, USA) "Studies in Natural Product Synthesis" |
9:25 pm - 9:30 pm | Discussion |
Thursday |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Accessing Bioactive Peptides and Proteins
/ RNA as Target and Modality |
| Discussion Leader: Donovan Chin (Novartis Institute for Biomedical Research, USA) |
9:00 am - 9:30 am | Richard Payne (University of Sydney, Australia) "Development of Ligation Chemistry for the Rapid Synthesis of Potent Anti-Thrombotic Proteins from Blood-Feeding Organisms" |
9:30 am - 9:35 am | Discussion |
9:35 am - 10:05 am | Hiroaki Suga (University of Tokyo, Japan) "Pseudo-Natural Products and Peptides for Therapeutic Applications" |
10:05 am - 10:10 am | Discussion |
10:10 am - 10:40 am | Coffee Break |
10:40 am - 11:10 am | Kevin Weeks (University of North Carolina at Chapel Hill, USA) "Chemical Microscopes and the RNA Structural Codes of Viruses and Cells" |
11:10 am - 11:15 am | Discussion |
11:15 am - 11:45 am | Matthew Disney (The Scripps Research Institute, USA) "Two-Dimensional Combinatorial Screening Enables Sequence-Based Design of Small Molecules Targeting RNA" |
11:45 am - 11:50 am | Discussion |
11:50 am - 12:25 pm | Matthew Stanton (Moderna Therapeutics, USA) "Messenger RNA as a Novel Therapeutic Approach" |
12:25 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 |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Toward Therapeutics |
| Discussion Leader: M.G. Finn (Georgia Institute of Technology, USA) |
7:30 pm - 8:05 pm | Emma Parmee (Merck, USA) "Early Discovery and the Quest for New Targets" |
8:05 pm - 8:10 pm | Discussion |
8:10 pm - 8:45 pm | Kimberly Stegmaier (Dana-Farber Cancer Institute, USA) "Targeting Cancer: At the Intersection of Chemistry, Functional Genomics, and Biology" |
8:45 pm - 8:50 pm | Discussion |
8:50 pm - 9:25 pm | Benjamin Cravatt (The Scripps Research Institute, USA) "Activity-Based Proteomics – Applications for Enzyme and Inhibitor Discovery" |
9:25 pm - 9:30 pm | Discussion |
Friday |
7:30 am - 8:30 am | Breakfast |
9:00 am | Departure |