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
Keynote Session: The Vanguard of Chemical Biology
Discussion Leader: Jennifer Prescher (University of California, Irvine, USA)
7:40 pm - 8:10 pm
Randy Peterson (Massachusetts General Hospital / Harvard University, USA)
"Behavior-Based Discovery of New Optochemical Genetic Tools"
8:10 pm - 8:15 pm
Discussion
8:15 pm - 8:45 pm
Daria Hazuda (Merck Research Laboratories, USA)
"Novel Approaches to Infectious Disease Targets"
8:45 pm - 8:50 pm
Discussion
8:50 pm - 9:25 pm
Dirk Trauner (New York University, USA)
"Optical Control of the Cytoskeleton"
9:25 pm - 9:30 pm
Discussion
Monday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Small Molecule Probes, Drug Candidates and New Approaches in Chemical Biology
Discussion Leader: Betsy Parkinson (University of Illinois at Urbana-Champaign, USA)
9:00 am - 9:30 am
Anna Mapp (University of Michigan, USA)
"Small Molecule Modulators of Conformationally Dynamic Protein Complexes"
9:30 am - 9:35 am
Discussion
9:35 am - 10:05 am
Richard Sparks (Incyte Corporation, USA)
"Fragment to Pharmacophore to Candidate: Invention of INCB054329, a Potent and Selective BRD Inhibitor in Clinical Trials for Oncology"
10:05 am - 10:10 am
Discussion
10:10 am - 10:40 am
Jonathan Morris (University of New South Wales, Australia)
"Developing Small Molecule Inhibitors of RNA Splicing Kinases for the Modulation of Protein Isoforms"
10:40 am - 10:45 am
Discussion
10:45 am - 11:15 am
Coffee Break
11:15 am - 11:45 am
Emily Balskus (Harvard University, USA)
"Deciphering the Human Microbiome Using Chemistry"
11:45 am - 11:50 am
Discussion
11:50 am - 12:05 pm
Benjamin Spangler (Novartis Institutes for Biomedical Research, USA)
"Molecular Probes for Determination of Sub-Cellular Compound Exposure in Gram-Negative Bacteria"
12:05 pm - 12:10 pm
Discussion
12:10 pm - 12:25 pm
Justin Rettenmaier (Whitehead Institute for Biological Research, USA)
"DELs in Cells: Phenotypic Screening with DNA-Encoded Cyclic Peptides"
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
Chemical Biology with Proteins, Mini-Proteins, and Peptides
Discussion Leader: Joshua Kritzer (Tufts University, USA)
7:30 pm - 8:05 pm
Albert Bowers (UNC Eshelman School of Pharmacy, USA)
"Chemoenzymatic Platforms for the Discovery of New Peptide Therapeutics"
8:05 pm - 8:10 pm
Discussion
8:10 pm - 8:45 pm
Brad Pentelute (Massachusetts Institute of Technology, USA)
"Homogenous Antibody Drug Conjugates Enabled by Cysteine Arylation"
8:45 pm - 8:50 pm
Discussion
8:50 pm - 9:25 pm
Alan Saghatelian (Salk Institute for Biological Studies, USA)
"Discovery and Characterization of Novel Microproteins"
9:25 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
Novel Chemistries and Methods for Chemical Biology and Therapeutics
Discussion Leader: Aaron Wright (Pacific Northwest National Laboratory, USA)
9:00 am - 9:30 am
Marcus Bantscheff (Cellzome / GlaxoSmithKline, Germany)
"Comprehensive Drug Target Profiling Using Complementary (Chemo-)proteomics Approaches"
9:30 am - 9:35 am
Discussion
9:35 am - 10:05 am
Emily Parker (Victoria University of Wellington, New Zealand)
"Unravelling and (Re)engineering Biosynthetic Pathways"
10:05 am - 10:10 am
Discussion
10:10 am - 10:40 am
Jennifer Prescher (University of California, Irvine, USA)
"Spying on Cellular Communication"
10:40 am - 10:45 am
Discussion
10:45 am - 11:15 am
Coffee Break
11:15 am - 11:30 am
Alison Narayan (University of Michigan, USA)
"Biocatalysis for Complex Molecule Synthesis"
11:30 am - 11:35 am
Discussion
11:35 am - 11:50 am
Shigeki Kiyonaka (Kyoto University, Japan)
"Chemogenetic Approach for Allosteric Activation of Neurotransmitter Receptors on Living Cells"
11:50 am - 11:55 am
Discussion
11:55 am - 12:25 pm
Corey Nislow (Genetic Networks, USA)
"The Cellular Response to Drugs Quantified by Fitness Profiling: A Genetic Networks' Perspective"
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
Chemical Biology: Phenotype, Target Engagement, and Mechanism of Action
Discussion Leader: Cynthia Chio (University of California, San Francisco, USA)
7:30 pm - 8:05 pm
Stewart Fisher (C4 Therapeutics, Inc., USA)
"It's About Time: Mechanistic PK-PD Models for Time-Dependent Inhibitors"
8:05 pm - 8:10 pm
Discussion
8:10 pm - 8:45 pm
Lyn Jones (Jnana Therapeutics, USA)
"Drug-Target Engagement in Live Cells"
8:45 pm - 8:50 pm
Discussion
8:50 pm - 9:25 pm
Christopher Vakoc (Cold Spring Harbor Laboratory, USA)
"Generating Resistance Alleles of Epigenetic Drug Targets"
9:25 pm - 9:30 pm
Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Novel Chemistries and Methods for Chemical Biology and High-Throughput Experimentation
Discussion Leader: Samuel Gerritz (Bristol-Myers Squibb, USA)
9:00 am - 9:30 am
Stevan Djuric (AbbVie, USA)
"Enabling Chemistry Technologies - Accelerators of Drug Discovery"
9:30 am - 9:35 am
Discussion
9:35 am - 10:05 am
Alexander Satz (Roche, Switzerland)
"Design and Application of DNA Encoded Libraries at Roche"
10:05 am - 10:10 am
Discussion
10:10 am - 10:40 am
Melodie Christensen (Merck, USA)
"High Throughput Experimentation in the Optimization of Metallaphotoredox Catalyzed Alpha-Hydroxy Arylation Reactions"
10:40 am - 10:45 am
Discussion
10:45 am - 11:20 am
Coffee Break
11:20 am - 11:50 am
Aleksandra Baranczak (AbbVie, USA)
"Approaches to Cellular Characterization of Small Molecule Protein Binders"
11:50 am - 11:55 am
Discussion
11:55 am - 12:25 pm
Anthony Keefe (X-Chem Pharmaceuticals, USA)
"Drug Discovery for Challenging Targets Using DNA-Encoded Chemistry"
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
7:00 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
Chemistry and Biology of Natural Products
Discussion Leader: Tarek Sammakia (University of Colorado Boulder, USA)
7:30 pm - 8:05 pm
Corinna Schindler (University of Michigan, USA)
"New Methods for the Synthesis of Biologically Active Molecules"
8:05 pm - 8:10 pm
Discussion
8:10 pm - 8:45 pm
Michael Burkart (University of California, San Diego, USA)
"Directing Biosynthesis Through Protein-Protein Interactions"
8:45 pm - 8:50 pm
Discussion
8:50 pm - 9:25 pm
Corey Stephenson (University of Michigan, USA)
"Redox Catalysis for Complex Molecule Synthesis"
9:25 pm - 9:30 pm
Discussion
Thursday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Bivalent Molecules and Other Novel Approaches to Control of Function
Discussion Leader: Lyn Jones (Jnana Therapeutics, USA)
9:00 am - 9:30 am
Jingwen Zhang (AstraZeneca, USA)
"Clinical Candidate AZD5153 Is a Novel Bivalent Inhibitor of BET Bromodomains"
9:30 am - 9:35 am
Discussion
9:35 am - 10:05 am
Rhamy Zeid (C4 Therapeutics, USA)
"Targeted Protein Degradation as a Novel Therapeutic Approach"
10:05 am - 10:10 am
Discussion
10:10 am - 10:40 am
David Spiegel (Yale University, USA)
"Bifunctional Molecules for Modulating Human Immune Responses"
10:40 am - 10:45 am
Discussion
10:45 am - 11:20 am
Coffee Break
11:20 am - 11:50 am
Yimon Aye (Cornell University / Weill Cornell Medicine, USA)
"'Stay on Target' — Targeting Kinetically Privileged First Responders in Electrophile Signaling"
11:50 am - 11:55 am
Discussion
11:55 am - 12:25 pm
M.G. Finn (Georgia Institute of Technology, USA)
"Low Throughput Studies of Reactivity to Enable High Throughput Applications"
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: Novel Therapeutics
Discussion Leader: Alan Saghatelian (Salk Institute for Biological Studies, USA)
7:30 pm - 8:05 pm
Phil Chamberlain (Celgene, USA)
"Expanding the Druggable Genome with Cereblon Modulators"
8:05 pm - 8:10 pm
Discussion
8:10 pm - 8:45 pm
Nathanael Gray (Dana Farber Cancer Institute, USA)
"Targeting Transcription Addiction in Cancer"
8:45 pm - 8:50 pm
Discussion
8:50 pm - 9:25 pm
Steve Haggarty (Harvard Medical School / Massachusetts General Hospital, USA)
"Probing Neurogenetic Disorders Using Patient-Specific Stem Cells and Chemogenomics"
9:25 pm - 9:30 pm
Discussion
Friday
7:30 am - 8:30 am
Breakfast
9:00 am
Departure