The Development of Chemical Probes to Decipher Biology

June 10 - 15, 2018

Chairs Paul R. Thompson and Erik C. Hett

Vice Chairs Jason E. Gestwicki and Paola Castaldi

Proctor Academy

204 Main Street

Andover, NH, US

Venue and Travel Information

Conference Description

The Bioorganic Chemistry Gordon Research Conference (GRC) was established in 1992 to bring together scientists pursuing challenges at the interface of chemistry and biology. Attendees from industry and academia meet annually to discuss the latest chemical tools that have been developed to modulate and interrogate biological complexity. The 2018 meeting will focus on liganding undruggable targets, targeting RNA with small molecules, chemical microbiology, the development of new chemical tools to unlock biology and translating small molecule probes into therapeutics. Conferees are encouraged to present posters. Poster presenters should submit an abstract with their applications on the GRC web site. A number of poster presenters will be invited to present short talks. As this meeting usually oversubscribes, submission of applications in early 2018 is strongly encouraged.

Related Meeting

This GRC will be held in conjunction with the "Bioorganic Chemistry (GRS)" Gordon Research Seminar (GRS). Those interested in attending both meetings must submit an application for the GRS in addition to an application for the GRC. Refer to the associated GRS program page for more information.

Conference Program

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	Covalent Inhibitors as Drugs Discussion Leader: Daniel Nomura (University of California, Berkeley, USA)
7:40 pm - 8:05 pm	Nathanael Gray (Dana Farber Cancer Institute, USA) "New Pharmacological Approaches to Kinase Inhibitor Discovery: Degradation, Allostery and Covalence"
8:05 pm - 8:10 pm	Discussion
8:10 pm - 8:25 pm	Sherry Niessen (Pfizer, USA) "Applying Chemical Biology Probes for the EGFRT790M Covalent Inhibitor Program"
8:25 pm - 8:30 pm	Discussion
8:30 pm - 8:45 pm	Bryan Dickinson (The University of Chicago, USA) "Chemical Approaches to Probe Signaling by Dynamic Proteome Lipidation"
8:45 pm - 8:50 pm	Discussion
8:50 pm - 9:05 pm	Nathanael Lintner (Pfizer, Inc., USA) "Selective Inhibition of Translation with Small Molecules"
9:05 pm - 9:10 pm	Discussion
9:10 pm - 9:25 pm	Jacqueline Blankman (Abide Therapeutics, USA) "Inhibition of Monoacylglycerol Lipase for the Treatment of Neurological Disorders"
9:25 pm - 9:30 pm	Discussion
Monday
7:30 am - 8:30 am	Breakfast
9:00 am - 12:30 pm	Chromatin Modifying Enzymes Discussion Leader: Champak Chatterjee (University of Washington, USA)
9:00 am - 9:30 am	James Bradner (Novartis Institutes for BioMedical Research, USA) "Targeting Epigenomic Complexes"
9:30 am - 9:40 am	Discussion
9:40 am - 10:10 am	Philip Cole (Harvard Medical School, USA) "Targeting Reversible Lys Modifications with Designed Small Molecules"
10:10 am - 10:20 am	Discussion
10:20 am - 10:50 am	Coffee Break
10:50 am - 11:20 am	Danica Fujimori (University of California, San Francisco, USA) "Regulation and Small Molecule Inhibition of Chromatin Demethylation"
11:20 am - 11:30 am	Discussion
11:30 am - 11:45 am	Jordan Meier (National Cancer Institute, NIH, USA) "An Expanded Landscape of Acetylation in Signaling from Chemoproteomics"
11:45 am - 11:50 am	Discussion
11:50 am - 12:05 pm	William Pomerantz (University of Minnesota, USA) "Fluorinated Proteins as Enabling Tools for Small Molecule Discovery in Epigenetics"
12:05 pm - 12:10 pm	Discussion
12:10 pm - 12:25 pm	Kabirul Islam (University of Pittsburgh, USA) "Protein and Small Molecule Engineering Towards a Programmable Chromatin Landscape"
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	Power Hour The GRC Power Hour is an optional informal gathering open to all meeting participants. It is designed to help address the challenges women face in science and support the professional growth of women in our communities by providing an open forum for discussion and mentoring. Organizer: Catherine Leimkuhler Grimes (University of Delaware, USA)
4:00 pm - 6:00 pm	Poster Session
6:00 pm - 7:00 pm	Dinner
7:30 pm - 9:30 pm	Liganding Undruggable Targets Discussion Leader: Raymond Moellering (University of Chicago, USA)
7:30 pm - 8:00 pm	Michelle Arkin (University of California, San Francisco, USA) "Site-Directed Screening: Harnessing Cysteines to Modulate Challenging Targets"
8:00 pm - 8:10 pm	Discussion
8:10 pm - 8:40 pm	Phil Chamberlain (Celgene, USA) "Expanding the Druggable Proteome Through Cereblon-Mediated Protein Degradation"
8:40 pm - 8:50 pm	Discussion
8:50 pm - 9:20 pm	Craig Crews (Yale University, USA) "PROTACs and Induced Protein Degradation: The 17-Year Old Overnight Phenomenon"
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	Chemical Microbiology Discussion Leader: Stavroula Hatzios (Yale University, USA)
9:00 am - 9:30 am	Suzanne Walker (Harvard Medical School, USA) "Using Genome-Wide Mutant Fitness Profiles to Decipher Compound Mechanism"
9:30 am - 9:40 am	Discussion
9:40 am - 10:10 am	Wilfred van der Donk (Howard Hughes Medical Institute / University of Illinois at Urbana-Champaign, USA) "Leader Peptide Guided Natural Product Biosynthesis"
10:10 am - 10:20 am	Discussion
10:20 am - 10:50 am	Coffee Break
10:50 am - 11:20 am	Sarah O'Connor (John Innes Centre, United Kingdom) "Harnessing the Chemistry of Alkaloid-Producing Plants"
11:20 am - 11:30 am	Discussion
11:30 am - 11:45 am	Louise Charkoudian (Haverford College, USA) "Capturing Transient Interactions of Proteins Involved in Natural Product Biosynthesis"
11:45 am - 11:50 am	Discussion
11:50 am - 12:05 pm	Sarah Slavoff (Yale University, USA) "Regulated Expression of the (Non-)Annotated Proteome"
12:05 pm - 12:10 pm	Discussion
12:10 pm - 12:25 pm	G. Ekin Atilla-Gokcumen (University at Buffalo, USA) "Non-Traditional Role of Lipids in Programmed Cell Death"
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 in Drug Discovery Discussion Leader: Catherine Leimkuhler Grimes (University of Delaware, USA)
7:30 pm - 8:00 pm	Steven Zimmerman (University of Illinois at Urbana-Champaign, USA) "New Approaches to the Discovery and Delivery of Agents Targeting RNA-Mediated Disease"
8:00 pm - 8:10 pm	Discussion
8:10 pm - 8:40 pm	Gitte Neubauer (Cellzome GmbH, Germany) "Chemistry Meets Omics: Understanding How Drugs Work"
8:40 pm - 8:50 pm	Discussion
8:50 pm - 9:05 pm	Kay Ahn (Janssen Research & Development, USA) "Chemical Biology Approach for Small Molecule Inhibitor Mechanism of Action Studies in Living Cells"
9:05 pm - 9:10 pm	Discussion
9:10 pm - 9:25 pm	Jacob Bush (GlaxoSmithKline, United Kingdom) "PhABits Shine Lght on Fragment-Protein Binding"
9:25 pm - 9:30 pm	Discussion
Wednesday
7:30 am - 8:30 am	Breakfast
9:00 am - 12:30 pm	Imaging and Optochemical Control Discussion Leader: Ellen Sletten (University of California, Los Angeles, USA)
9:00 am - 9:30 am	Jin Zhang (University of California, San Diego, USA) "Illuminating the Biochemical Activity Architecture of the Cell"
9:30 am - 9:40 am	Discussion
9:40 am - 10:10 am	Dirk Trauner (New York University, USA) "Optical Control of GPCRs and Kinases"
10:10 am - 10:20 am	Discussion
10:20 am - 10:40 am	Coffee Break
10:40 am - 11:10 am	Alexander Deiters (University of Pittsburgh, USA) "Optical Control of Protein Function in Cells and Animals"
11:10 am - 11:20 am	Discussion
11:20 am - 11:35 am	Jennifer Heemstra (Emory University, USA) "Harnessing Nucleic Acid Molecular Recognition for Fluorescence-Based Biomolecular Imaging"
11:35 am - 11:40 am	Discussion
11:40 am - 11:55 am	Alison Narayan (University of Michigan, USA) "Biocatalysis: Harnessing the Power of Nature's Tools to Build Complex Molecules"
11:55 am - 12:00 pm	Discussion
12:00 pm - 12:10 pm	Kevin Bicker (Middle Tennessee State University, USA) "Development of Short Peptoids as Antifungal Agents Against C. neoformans"
12:10 pm - 12:15 pm	Discussion
12:15 pm - 12:25 pm	Alicia Angelbello (The Scripps Research Institute, USA) "Small Molecule Cleavage of a Toxic RNA Repeat"
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	Modulating Protein Function Discussion Leader: Rongsheng (Ross) Wang (Temple University, USA)
7:30 pm - 8:00 pm	Benjamin Davis (University of Oxford, United Kingdom) "Sugars and Proteins"
8:00 pm - 8:10 pm	Discussion
8:10 pm - 8:40 pm	Herbert Waldmann (Max Planck Institute of Molecular Physiology, Germany) "Pseudo Natural Products for Phenotypic Small Molecule Discovery"
8:40 pm - 8:50 pm	Discussion
8:50 pm - 9:20 pm	Elizabeth Sattely (Stanford University, USA) "Discovery and Engineering Plant Chemistry"
9:20 pm - 9:30 pm	Discussion
Thursday
7:30 am - 8:30 am	Breakfast
9:00 am - 12:30 pm	Targeting RNA with Small Molecules Discussion Leader: Amanda Garner (University of Michigan, USA)
9:00 am - 9:30 am	Matthew Disney (The Scripps Research Institute, USA) "Sequence-Based Design of Small Molecules Targeting RNA"
9:30 am - 9:40 am	Discussion
9:40 am - 10:10 am	Kevin Weeks (University of North Carolina at Chapel Hill, USA) "Discovering the Pervasive Roles for Structure in ncRNA and mRNA Function"
10:10 am - 10:20 am	Discussion
10:20 am - 10:50 am	Coffee Break
10:50 am - 11:20 am	Jennifer Petter (Arrakis Therapeutics, USA) "RNA-Targeted Small Molecules: A Problem in Drug Discovery"
11:20 am - 11:30 am	Discussion
11:30 am - 11:45 am	Amanda Hargrove (Duke University, USA) "Deciphering Patterns in Selective Small Molecule: RNA Interactions"
11:45 am - 11:50 am	Discussion
11:50 am - 12:05 pm	Jay Schneekloth (National Cancer Institute, NIH, USA) "Targeting Structurally and Functionally Diverse RNAs with Druglike Small Molecules"
12:05 pm - 12:10 pm	Discussion
12:10 pm - 12:25 pm	John Howe (Merck & Co., USA) "Selective Small Molecule Inhibition of an RNA Structural Element"
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	New Chemical Tools to Unlock Biology Discussion Leader: Darci Trader (Purdue University, USA)
7:30 pm - 8:00 pm	Yimon Aye (École Polytechnique Fédérale de Lausanne, Switzerland) "A Twist in the Tail? Precision Electrophile Sensing Guides Isoform-Selective Covalent Ligand Evolution"
8:00 pm - 8:10 pm	Discussion
8:10 pm - 8:40 pm	Ming Hammond (University of California, Berkeley, USA) "Riboswitching on the Light: Illuminating the Single-Cell Biology of Bacterial Signals"
8:40 pm - 8:50 pm	Discussion
8:50 pm - 9:20 pm	Dorothea Fiedler (Leibniz-Institute for Molecular Pharmacology (FMP), Germany) "Inositol Pyrophosphate Signaling Revealed with Chemical Tools"
9:20 pm - 9:30 pm	Discussion
Friday
7:30 am - 8:30 am	Breakfast
9:00 am	Departure