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 Staff / Welcome and Introduction from the Chairs
7:40 pm - 9:30 pm
Keynote Session: Analysis of Chemical and Biological Complexity at Scale
Discussion Leader: Srinivas Chamakuri (Baylor College of Medicine, United States)
7:40 pm - 8:30 pm
Petra Dittrich (ETH Zurich, Switzerland)
"Multimodal High-Throughput Analysis Enabled by Sessile Droplet Arrays"
8:30 pm - 8:35 pm
Discussion
8:35 pm - 9:25 pm
Polly Fordyce (Stanford University, United States)
"Microfluidics for High-Throughput and Quantitative Biophysics and Biochemistry"
9:25 pm - 9:30 pm
Discussion
Monday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
RNA Structure and Drug Discovery
Discussion Leader: MariJean Eggen (Eli Lilly, United States)
9:00 am - 9:30 am
Amanda Hargrove (Duke University, United States)
"Modulating the Conformation and Function of Disease-Relevant RNA With Small Molecules"
9:30 am - 9:35 am
Discussion
9:35 am - 9:50 am
Liron Bar-Peled (MGH Cancer Center and Harvard Medical School, United States)
"A Pan-Cancer DrugMap Reveals Heterogeneity in Covalent Cysteine Targeting"
9:50 am - 9:55 am
Discussion
9:55 am - 10:25 am
Kerrie Spencer (Merck, United States)
"Small Molecule Targeting of Xist RNA Disrupts Repeat A Structure and X-Chromosome Inactivation"
10:25 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Jessica Brown (University of Notre Dame, United States)
"The MALAT1 RNA Triple Helix: What Do We Know about this Alluring Drug Target"
11:30 am - 11:35 am
Discussion
11:35 am - 11:50 am
Jarrett Pelton (University of North Carolina, United States)
"Cheminformatics-Guided Cell Free Biosynthetic Exploration of Peptide Natural Products"
11:50 am - 11:55 am
Discussion
11:55 am - 12:25 pm
Jennifer Petter (Arrakis Therapeutics, United States)
"A Structure-Based Approach to RNA-targeted Small Molecules"
12:25 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 diversity and inclusion in the scientific workplace by providing a safe environment for informal and meaningful conversations amongst colleagues of all career stages. The program supports the professional growth of all members of our communities, including ethnicity, race and/or gender identity by providing an open forum for discussion and mentoring.
Organizers: Jennifer Heemstra (Washington University in St. Louis, United States) and Kerrie Spencer (Merck, United States)
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Leveraging Artificial Intelligence for Privileged Tool Development
Discussion Leader: William Pomerantz (University of Minnesota, United States)
7:30 pm - 8:00 pm
Jean-Louis Reymond (University of Bern, Switzerland)
"Chemical Space Inspired Design of Small Molecules and Peptides"
8:00 pm - 8:05 pm
Discussion
8:05 pm - 8:15 pm
Kuangbiao Liao (Guangzhou Laboratory / AIChemEco Inc., China)
"Building a Reaction Database Using High-Throughput Technology: Enabling AI Chemistry"
8:15 pm - 8:20 pm
Discussion
8:20 pm - 8:50 pm
Nessa Carson (AstraZeneca, United Kingdom)
"Championing 'Digital' at AstraZeneca"
8:50 pm - 8:55 pm
Discussion
8:55 pm - 9:25 pm
Thomas Girke (University of California, Riverside, United States)
"Profiling Genome-wide Effects of Small Molecules with Gene Expression Signature Searching"
9:25 pm - 9:30 pm
Discussion
Tuesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Reaction Scouting for High-Throughput Chemistry and DELs
Discussion Leader: Alexander Satz (WuXi AppTec, Germany)
9:00 am - 9:25 am
Dennis Gillingham (University of Basel, Switzerland)
"Methods to Record and Amplify Signals During DNA Encoded Library Selections"
9:25 am - 9:30 am
Discussion
9:30 am - 9:55 am
Charles Hendrick (Janssen Research & Development, United States)
"High-Throughput Experimentation to Accelerate Modality Agnostic Drug Discovery"
9:55 am - 10:00 am
Discussion
10:00 am - 10:30 am
Group Photo / Coffee Break
10:30 am - 10:55 am
Dipannita Kalyani (Merck & Co., Inc., United States)
"Accelerating Drug Discovery: Innovations in High-Throughput Experimentation"
10:55 am - 11:00 am
Discussion
11:00 am - 11:25 am
Alexander Domling (Palacký University Olomouc, Czech Republic)
"Automation + Miniaturization = Acceleration: Acoustic Droplet Ejection-Enabled HT Synthetic Chemistry"
11:25 am - 11:30 am
Discussion
11:30 am - 11:55 am
Andrew MacConnell (1859 inc., United States)
"Generating QSAR for ML Guided Lead Development from Activity-based DEL Platform"
11:55 am - 12:00 pm
Discussion
12:00 pm - 12:25 pm
Alexander Buitrago Santanilla (GSK, United States)
"Application of Nanoscale Direct to Biology Platform at GSK"
12:25 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
Expanding and Understanding Diversity: DELs and Cheminformatics
Discussion Leader: Zhicai Shi (Janssen, Pharmaceutical Companies of Johnson & Johnson, United States)
7:30 pm - 7:55 pm
Tessa Epstein (University of Michigan, United States)
"Tricyclic Azaphilones are Potent and Specific Inhibitors of HuR-mRNA Interactions"
7:55 pm - 8:00 pm
Discussion
8:00 pm - 8:25 pm
Carol Mulrooney (GSK, United States)
"Expanding the Chemical Space of DNA-Encoded Libraries in Two and Three Dimensions"
8:25 pm - 8:30 pm
Discussion
8:30 pm - 8:55 pm
Paige Dickson (X-Chem, United States)
"Employing DNA-encoded Libraries to Identify Novel Chemical Equity for PPIs and Beyond"
8:55 pm - 9:00 pm
Discussion
9:00 pm - 9:25 pm
Peter Kutchukian (Novartis Institutes for Biomed. Research, United States)
"Pushing the Boundaries of Chemical Space: DEL, Virtual Libraries, and Generative Chemistry"
9:25 pm - 9:30 pm
Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Chemical Probes and Phenotypic Cellular Assays
Discussion Leader: Damian Young (Baylor College of Medicine, United States)
9:00 am - 9:30 am
Jason Sello (University of California, San Francisco, United States)
"Leveraging Behavior as a Phenotype in High Throughput Screening"
9:30 am - 9:35 am
Discussion
9:35 am - 9:50 am
William Pomerantz (University of Minnesota, United States)
"New Chemical Probes for the Nucleosome Remodeling Factor, NURF, an Emerging Therapeutic Target in Adult and Pediatric Cancers"
9:50 am - 9:55 am
Discussion
9:55 am - 10:25 am
Jennifer Heemstra (Washington University in St. Louis, United States)
"Harnessing Nature’s Molecular Recognition Capabilities for High-Throughput Profiling of A-to-I RNA Editing"
10:25 am - 10:30 am
Discussion
10:30 am - 11:05 am
Coffee Break
11:05 am - 11:35 am
Heidi Greulich (Broad Institute, United States)
"Mechanism of Action of Velcrin Small Molecules"
11:35 am - 11:40 am
Discussion
11:40 am - 11:50 am
Malliga Iyer (NIAAA/NIH, United States)
"Development of a Unified Chemical Platform to Probe Polypharmacology: Case Study Leading to a Clinical Candidate"
11:50 am - 11:55 am
Discussion
11:55 am - 12:25 pm
Jacquin Niles (Massachusetts Institute of Technology, United States)
"Scalable Chemogenomics Through Target-Encoded Phenotypic Screens for Antimalarial Drug Discovery"
12:25 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
Inflammasomes: Dissecting and Interrogating Inflammasome Pathways
Discussion Leader: Amber Hackler (Merck, United States)
7:30 pm - 8:00 pm
Darci Trader (University of California- Irvine, United States)
"Studies of the Role of the Immunoproteasome Under Inflammatory Conditions"
8:00 pm - 8:05 pm
Discussion
8:05 pm - 8:35 pm
Albert Bowers (University of North Carolina at Chapel Hill, United States)
"Building on Natural Product Motifs for Cyclic Peptide Inhibitor Discovery"
8:35 pm - 8:40 pm
Discussion
8:40 pm - 8:50 pm
Seiya Kitamura (Albert Einstein College of medicine, United States)
"A Universal High-Throughput Platform to Develop Chemical Probes and Drug Candidates"
8:50 pm - 8:55 pm
Discussion
8:55 pm - 9:25 pm
Daniel Bachovchin (Memorial Sloan Kettering Cancer Center, United States)
"Activation of the NLRP1 Inflammasome"
9:25 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(s); Complete the GRC Evaluation Forms; Discuss Future Dates and Venue; Election of the Next Vice Chair(s)
9:00 am - 12:30 pm
Cutting-Edge Omics Tools and Integration into Drug Discovery
Discussion Leader: Albert Bowers (University of North Carolina at Chapel Hill, United States)
9:00 am - 9:30 am
Christian Münch (Goethe University Frankfurt, Germany)
"Dynamic Proteomics for Exploring Protein Homeostasis"
9:30 am - 9:35 am
Discussion
9:35 am - 9:50 am
Hui Jing (AbbVie, United States)
"An Automated High-throughput Affinity Capture Mass Spectrometry Assay with Data-Independent Acquisition for Kinase Inhibitor Profiling"
9:50 am - 9:55 am
Discussion
9:55 am - 10:25 am
Xiaoyu Shi (University of California, Irvine, United States)
"High-Throughput Superresolution Imaging for Subcellular Phenotype Analysis and Drug Assessment"
10:25 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Keriann Backus (University of California, Los Angeles, United States)
"Custom Isobaric Strategies for Quantitative Chemoproteomics"
11:30 am - 11:35 am
Discussion
11:35 am - 11:50 am
Katherine McPhie (The Francis Crick Institute, United Kingdom)
"Chemical Biology Approaches to Explore the Ligandability of TRIM E3 Ligases"
11:50 am - 11:55 am
Discussion
11:55 am - 12:25 pm
Christopher Parker (Scripps Research, United States)
"Proteome-Wide Ligand and Target Discovery in Cells"
12:25 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: Expanding Novel Platforms to Probe Biological Pathways
Discussion Leader: Mark Fitzgerald (Nested Therapeutics, United States)
7:30 pm - 8:00 pm
Stacy Malaker (Yale University, United States)
"Glycosite Mapping and Structural Dynamics of TIM Family Immune Checkpoints Enabled by Mucinase SME"
8:00 pm - 8:05 pm
Discussion
8:05 pm - 8:15 pm
Callie Fredlender (UC Irvine, United States)
"DELs, Cells, and Gels: Microsphere Culture for Cellular Activity-Based DEL Screening"
8:15 pm - 8:20 pm
Discussion
8:20 pm - 8:50 pm
Ingrid Wertz (Lyterian Therapeutics, United States)
"Co-Opting the Ubiquitin System for Therapeutic Benefit"
8:50 pm - 8:55 pm
Discussion
8:55 pm - 9:25 pm
Sara Buhrlage (Dana-Farber Cancer Institute, United States)
"Accelerating Inhibitor Discovery for Deubiquitinases"
9:25 pm - 9:30 pm
Discussion
Friday
7:30 am - 8:30 am
Breakfast
9:00 am
Departure